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Rosiglitazone (BRL 49653) Agonista PPARγ

Name: Rosiglitazone (BRL 49653)
Brand: Selleck Chemicals
SKU: S2556
Rating: 5 (76 reviews)

N. Cat.S2556

Il Rosiglitazone è un potente agente antiperglicemico e un potente sensibilizzatore all'insulina tiazolidinedionico con IC50 di 12, 4 e 9 nM per adipociti di ratto, 3T3-L1 e umani, rispettivamente. Il Rosiglitazone è un ligando puro di PPAR-gamma e non ha azione di legame con PPAR-alpha. Il Rosiglitazone modula i TRP channels e induce l'autophagy. Il Rosiglitazone previene la ferroptosis.

Rosiglitazone (BRL 49653) PPAR agonista Chemical Structure

Struttura chimica

Peso molecolare: 357.43

Vai a

Controllo Qualità

Lotto: Purezza: 99.99%

99.99

Target correlati	Dehydrogenase HSP Transferase P450 (e.g. CYP17) PDE phosphatase Vitamin Carbohydrate Metabolism Mitochondrial Metabolism Drug Metabolite
Altro PPAR Inibitori	T0070907 GW9662 GW6471 WY-14643 (Pirinixic Acid) GSK3787 GW0742 AZ6102 Harmine Astaxanthin Eupatilin

Coltura cellulare, trattamento e concentrazione di lavoro

Linee cellulari	Tipo di saggio	Concentrazione	Tempo di incubazione	Descrizione dellattività	PMID
HepG2	Function assay			Effective concentration against human PPARgamma expressed in HepG2 cells, EC50=0.02 μM	15801817
CV-1	Function assay			In vitro transcriptional activation of Peroxisome proliferator activated receptor gamma (PPAR) expressed in CV-1 cells, EC50 = 0.06 μM.	8576907
CV-1	Function assay			Activation of peroxisome proliferator activated receptor gamma measured by induction of 50% of maximum alkaline phosphatase activity, transfection assay in CV-1 cells, EC50 = 0.08913 μM.	9836620
3T3-L1	Function assay			Stimulation of adipogenesis in 3T3-L1 cells is expressed as concentration equivalent to the [ 1-14C] uptake counts after treatment with 0.2 ug/mL troglitazone, EC = 0.09 μM.	10956213
CV-1	Function assay			Maximal reporter activity against human Peroxisome proliferator activated receptor gamma Gal4 chimeric in transiently transfected CV-1 cells by functional assay., EC50 = 0.043 μM.	11720854
COS1	Function assay			Agonistic activity was determined in COS1 cells transfected with GAL 4-PPAR gamma receptor, EC50 = 0.021 μM.	12617924
COS1	Function assay			In vitro agonist activity tested for transactivation in human PPAR gamma-Gal4 chimeric COS-1 cells, EC50 = 0.02 μM.	12729668
COS1	Function assay			In vitro transactivation of human peroxisome proliferator activated receptor gamma measured in PPAR-GAL4 chimeric COS-1 cells, EC50 = 0.02 μM.	12873517
CV-1	Function assay			In vitro evaluation against RXR-alpha/PPAR-gamma in CV-1 cells by cotransfection assay was determined, EC50 = 0.325 μM.	12954061
3T3-L1	Function assay			Effective concentration for enhancement of insulin-induced triglyceride accumulation in 3T3-L1 cells, EC30 = 0.02 μM.	14505644
HepG2	Function assay			Effective concentration against human PPARgamma expressed in HepG2 cells, EC50 = 0.039 μM.	16107150
U2OS	Function assay			Effect on PPARgamma transactivation activity in U2OS cells, EC50 = 0.03 μM.	16300944
Huh7	Function assay			Functional activity at human PPAR gamma in Huh7 cells by transactivation assay, EC50 = 0.22 μM.	16366601
Huh7	Function assay			Effect on PPAR gamma transactivation activity in Huh7 cells, EC50 = 0.22 μM.	16451087
HEK293	Function assay			Agonist activity at PPARgamma expressed in HEK293 cells assessed as induction of receptor interaction with steroid receptor coactivator-1 by EYFP based reporter gene assay	16680159
HEK293	Function assay			Agonist activity at PPARgamma expressed in HEK293 cells assessed as induction of receptor interaction with retinoid X-receptor alpha by EYFP based reporter gene assay	16680159
CV1	Function assay			Transactivation of PPARgamma in CV1 cells, EC50 = 0.076 μM.	16821769
NIH3T3	Function assay			Activity at human PPAR gamma transfected in NIH3T3 cells by luciferase activity assay, EC50 = 0.32 μM.	16854085
CV1	Function assay			Transactivation of human PPARgamma in CV1 cells by luciferase reporter gene assay, EC50 = 0.308 μM.	16970391
HepG2	Function assay			Agonist activity at human PPAR gamma in a HepG2 cells by PPAR-GAL4 transactivation assay, EC50 = 0.158 μM.	16973358
HepG2	Function assay			Agonist activity at human PPAR gamma in HepG2 cells by PPAR-GAL4 transactivation assay, EC50 = 0.158 μM.	16979341
CV1	Function assay			Activity at human PPARgamma in CV1 cells, EC50 = 0.308 μM.	17005394
Huh7	Function assay			Activity at human PPAR gamma in Huh7 cells by transactivation assay, EC50 = 0.22 μM.	17034149
CV1	Function assay			Agonist activity at PPARgamma in CV1 cells by transactivation assay, EC50 = 0.308 μM.	17129725
HepG2	Function assay			Agonist activity at human PPARgamma in HepG2 cells by PPAR-GAL4 transactivation assay, EC50 = 0.082 μM.	17157019
HEK293	Function assay			Agonist activity at PPARgamma receptor expressed in HEK293 cells by GAL4 transactivation assay, EC50 = 0.035 μM.	17292606
HEK293	Function assay			Activity at human adipose tissue PPAR gamma expressed in HEK293 cells by PPAR-GAL4 transactivation assay, EC50 = 0.31 μM.	17343371
L6	Function assay			Effect on fatty acid oxidation in rat L6 cells, EC50 = 5 μM.	17343371
HepG2/C3A	Function assay			Activation of human PPARgamma ligand binding domain-mediated transcriptional activity in human HepG2/C3A cells co-transfected with fused Gal4-LBD by cotransfection assay, EC50 = 0.0038 μM.	17403688
CV1	Function assay		24 hrs	Agonist activity at human PPARgamma in CV1 cells by GAL4 transactivation assay after 24 hrs, EC50 = 0.03 μM.	17507225
CV1	Function assay		24 hrs	Agonist activity at human PPARalpha in CV1 cells by GAL4 transactivation assay after 24 hrs, EC50 = 3.46 μM.	17507225
NIH3T3	Function assay			Agonist activity at human PPARgamma expressed in NIH3T3 cells by GAL4 transactivation assay, EC50 = 0.32 μM.	17624777
HEK293	Function assay			Agonist activity at PPARgamma expressed in HEK293 cells assessed as aP2 gene induction, EC50 = 0.12 μM.	18029176
HEK293	Function assay			Agonist activity at PPARgamma expressed in HEK293 cells by GAL4 transactivation assay, EC50 = 0.19 μM.	18029176
CV1	Function assay			Agonist activity at human PPARgamma expressed in CV1 cells by receptor transactivation assay, EC50 = 0.308 μM.	18029178
HEK293	Function assay			Agonist activity at PPARgamma in HEK293 cells by GAL4 transactivation assay, EC50 = 0.045 μM.	18291645
U2OS	Function assay			Agonist activity at human PPARgamma in U2OS cells by transactivation assay, EC50 = 0.02 μM.	18329751
HepG2	Function assay			Agonist activity at human PPARgamma expressed in HepG2 cells by GAL4 transactivation assay, EC50 = 0.223 μM.	18394907
HepG2	Function assay			Agonist activity at PPARgamma expressed in human HepG2 cells assessed as induction of receptor transactivation by reporter gene assay relative to control, EC50 = 0.05 μM.	18625559
RAW264.7	Function assay			Suppression of LPS/IFN-gamma-stimulated NO production in mouse RAW264.7 cells, IC50 = 17.5 μM.	18809325
CV1	Function assay			Agonist activity at human PPARgamma ligand binding domain expressed in african green monkey CV1 cells co-transfected with fused Gal4-DBD by transactivation assay, EC50 = 0.033 μM.	18826205
CV1	Function assay			Agonist activity at human PPARalpha ligand binding domain expressed in african green monkey CV1 cells co-transfected with fused Gal4-DBD by transactivation assay, EC50 = 3.46 μM.	18826205
HepG2	Function assay			Agonist activity at human PPARalpha ligand binding domain expressed in human HepG2 cells co-transfected with Gal4 by luciferase reporter gene assay, EC50 = 0.039 μM.	18835719
HepG2	Function assay			Agonist activity at human PPARgamma ligand binding domain expressed in human Hep G2 cells co-transfected with Gal4-DBD by luciferase reporter gene assay, EC50 = 0.04 μM.	19053776
HeLa	Function assay			Agonist activity at PPARgamma ligand binding domain expressed in human HeLa cells co-transfected with Gal4-DBD assessed as transcriptional activation by Gal4 response element-driven luciferase reporter gene assay, EC50 = 0.015 μM.	19275963
BL21	Function assay			Displacement of radio labeled 2(S)-(2-benzoyl-phenylamino)-3-{4-[1,1-ditritio-2-(5-methyl-2-phenyl-oxazol-4-yl)-ethoxy]-phenyl}-propionic acid from GST-fused human PPARgamma expressed in Escherichia coli BL21 cells by scintillation proximity assay, IC50 = 0.45 μM.	19349176
BHK21	Function assay			Agonist activity at human PPARgamma expressed in BHK21 cells assessed as SEAP activity by luciferase reporter transactivation assay, EC50 = 0.45 μM.	19349176
COS1	Function assay		48 hrs	Agonist activity at human recombinant PPARgamma expressed in COS1 cells co-expressing GAL4 assessed as transcriptional activity after 48 hrs by luciferase reporter gene assay, EC50 = 0.02 μM.	19507861
COS1	Function assay			Agonist activity at human PPARgamma receptor expressed in african green monkey COS1 cells co-transfected with fused yeast Gal4-DBD by transactivation assay, EC50 = 0.02 μM.	19530681
U2OS	Function assay			Agonist activity at human PPARgamma expressed in U2OS cells by luciferase transactivation assay, EC50 = 0.05 μM.	19574056
MCF7	Function assay	0.1 uM	24 hrs	Activation of human PPAR-gamma-dependent transcription expressed in human MCF7 cells assessed as induction of PPRE-reporter gene expression at 0.1 uM after 24 hrs by dual luciferase reporter gene assay relative to rosiglitazone	19719236
HepG2	Function assay			Agonist activity at GAL4-tagged human PPARgamma ligand binding domain expressed in human HepG2 cells assessed as receptor transactivation by luciferase reporter gene assay, EC50 = 0.039 μM.	19775169
HepG2	Function assay			Agonist activity at human PPARgamma expressed in HepG2 cells by GAL4 transactivation assay, EC50 = 0.223 μM.	19783444
COS7	Function assay			Agonist activity at human recombinant PPARgamma1 LBD expressed in african green monkey COS7 cells coexpressing GAL4 by luciferase reporter gene transactivation assay, EC50 = 0.03 μM.	20138762
COS7	Function assay			Agonist activity at human recombinant PPARgamma2 LBD expressed in african green monkey COS7 cells coexpressing GAL4 by luciferase reporter gene transactivation assay, EC50 = 0.1 μM.	20138762
HEK	Function assay			Agonist activity at human GAL4-tagged PPARgamma chimeric receptor expressed in HEK cells by transactivation assay, EC50 = 0.035 μM.	20299214
HEK	Function assay			Agonist activity at human GAL4-tagged PPARalpha chimeric receptor expressed in HEK cells by transactivation assay, EC50 = 10.58 μM.	20299214
CHO-K1	Function assay			Partial agonist activity at human PPARgamma-LBD expressed in CHO-K1 cells co-transfected with GAL4 assessed as luciferase activity by transactivation assay, EC50 = 0.1 μM.	20527969
3T3L1	Function assay		7 days	Induction of adipogenesis in mouse 3T3L1 cells assessed as increase in lipid accumulation after 7 days by Oil red O staining	20527969
HEK293T	Function assay	1 uM	24 hrs	Partial agonist activity at human PPARgamma-LBD expressed in HEK293T cells assessed as induction of receptor transactivation at 1 uM after 24 hrs by luciferase reporter gene assay	21030263
CV1	Function assay			Transactivation of Gal4-fused human PPARgamma DNA binding domain expressed in african green monkey CV1 cells by luciferase reporter gene assay, EC50 = 0.1 μM.	21112784
HEK293	Function assay		16 to 20 hrs	Transactivation of Gal4-fused human PPARgamma expressed in HEK293 cells after 16 to 20 hrs by luciferase reporter gene assay, EC50 = 0.043 μM.	21128600
HepG2	Function assay	10 umol/L	24 hrs	Increase in glucose consumption in human HepG2 cells at 10 umol/L after 24 hrs relative to control	21256748
HepG2	Function assay			Transactivation of human PPARgamma expressed in human HepG2 cells co-transfected with PPRE3-TK-Luc by luciferase reporter gene assay, EC50 = 0.05 μM.	21450468
HepG2	Function assay			Agonist activity at PPARgamma receptor expressed in human HepG2 cells by PPRE-luciferase reporter gene assay, EC50 = 0.01 μM.	21482446
CV1	Function assay		40 hrs	Agonist activity at human PPARgamma-LBD expressed in CV1 cells co-transfected with Gal4 after 40 hrs by luciferase based transactivation assay, EC50 = 0.1 μM.	21515063
3T3L1	Function assay	10 uM		Increase in adiponectin mRNA levels in TNFalpha-induced mouse 3T3L1 cells pretreated at 10 uM before TNF-alpha challenge relative to control	21851089
COS7	Function assay			Modulation of human PPARgamma-LBD expressed in african green monkey COS7 cells co-transfected with Gal4 assessed as activation of transactivation activity by luciferase assay, EC50 = 0.043 μM.	21873070
Sf21	Function assay			Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake, IC50 = 6.4 μM.	21965623
Sf21	Function assay			Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake, IC50 = 40 μM.	21965623
COS-1	Function assay		24 hrs	Agonist activity at human PPARgamma ligand binding domain expressed in COS-1 cells after 24 hrs by luciferase reporter gene-based luminometric analysis, EC50 = 0.048 μM.	22051054
COS1	Function assay			Binding affinity to human wild type PPARgamma LBD expressed in COS1 cells co-expressing GAL4 by scintillation proximity assay	22070604
HepG2	Function assay		20 hrs	Agonist activity at human GAL4-fused PPARgamma ligand binding domain expressed in HepG2 cells after 20 hrs by luciferase reporter gene transactivation assay, EC50 = 0.02 μM.	22081932
BL21 DE3	Function assay			Displacement of [3H]rosiglitazone from N-terminal His-tagged human PPARgamma ligand binding domain expressed in Escherichia coli BL21 DE3 cells by scintillation proximity assay, Ki = 0.074 μM.	22081932
COS1	Function assay		24 hrs	Transactivation of human full length PPARgamma expressed in COS1 cells co-transfected with RXRalpha after 24 hrs by luciferase reporter gene assay, EC50 = 0.12 μM.	22197396
MG-63	Function assay			Agonist activity at human PPARgamma expressed in MG-63 cells by reporter gene-based transactivation assay, EC50 = 0.011 μM.	22225641
293H DA	Function assay		16 hrs	Agonist activity at PPARgamma LBD in human 293H DA cells after 16 hrs by TR-FRET activation reporter assay, EC50 = 0.0024 μM.	22582973
MG-63	Function assay		24 hrs	Modulation of full-length human pSG5-fused PPARgamma expressed in MG-63 cells co-expressing pGV-P2-PPRE after 24 hrs by luciferase reporter gene based transactivation assay, EC50 = 0.011 μM.	22727448
Ac2F	Function assay	0.1 to 10 uM	6 hrs	Agonist activity at PPARgamma in rat Ac2F cells assessed as luciferase activity at 0.1 to 10 uM after 6 hrs by reporter gene assay	22819190
HepG2	Function assay			Transactivation of GAL4-fused PPARgamma ligand binding domain transfected in human HepG2 cells by luciferase reporter gene assay, EC50 = 0.1 μM.	22934537
THP1	Function assay	100 uM	3 hrs	Transactivation of PPARgamma in human THP1 cells assessed as decrease in LPS-induced MCP1 mRNA expression at 100 uM preincubated for 3 hrs prior to LPS challenge measured after 18 hrs by RT-PCR analysis relative to untreated control	22934537
THP1	Function assay	100 uM	3 hrs	Transactivation of PPARgamma in human THP1 cells assessed as decrease in LPS-induced IL6 mRNA expression at 100 uM preincubated for 3 hrs prior to LPS challenge measured after 18 hrs by RT-PCR analysis relative to untreated control	22934537
HepG2	Function assay	10 uM	24 hrs	Reduction of glucose consumption in insulin-resistant human HepG2 cells at 10 uM after 24 hrs by glucose oxidase method in presence of 0.1 uM of insulin	23025244
HepG2	Function assay	10 uM	24 hrs	Reduction of glucose consumption in insulin-resistant human HepG2 cells at 10 uM after 24 hrs by glucose oxidase method in presence of 22.2 mM of glucose	23025244
HepG2	Function assay		20 hrs	Transactivation of GAL4-fused human PPARgamma ligand binding domain expressed in HepG2 cells after 20 hrs by luciferase reporter gene assay, EC50 = 0.039 μM.	23171045
L02	Function assay		24 hrs	Agonist activity at PPARgamma-LBD expressed in human L02 cells co-expressing pGL3-SV40-GAL4 after 24 hrs by luciferase reporter gene based transactivation assay, EC50 = 0.9 μM.	23186307
HEK293	Function assay		48 hrs	Agonist activity at human PPARgamma expressed in HEK293 cells cotransfected with PPREx4-TK-luc assessed as activation of luciferase activity measured after 48 hrs by transactivation assay, EC50 = 43.71 μM.	23265844
HEK293	Function assay	10 uM		Transactivation of PPARgamma (unknown origin) expressed in HEK293 cells co-transfected with AP2-PPRE at 10 uM by luciferase reporter gene assay	23273519
HEK293	Function assay			Agonist at human PPARgamma LBD expressed in human HEK293 cells cotransfected with GAL4-Luc assessed as transcriptional activation by luciferase reporter gene assay, EC50 = 0.004 μM.	23286787
HEK293	Function assay		24 hrs	Transactivation of GAL4 DBD-fused human PPARgamma-LBD expressed in HEK293 cells after 24 hrs by luciferase reporter gene assay, EC50 = 0.1 μM.	23294830
CMT93	Function assay	10 uM	30 mins	Induction of PPAR-gamma promoter activity in LPS-stimulated mouse CMT93 cells at 10 uM preincubated for 30 mins before LPS-challenge measured after 6 hrs post challenge by luciferase reporter gene assay	23416190
HepG2	Function assay			Agonist activity at GAL4-fused PPARgamma M463A mutant (unknown origin) expressed in human HepG2 cells by transactivation assay, EC50 = 0.002 μM.	23502212
HepG2	Function assay			Agonist activity at GAL4-fused PPARgamma (unknown origin) expressed in human HepG2 cells by transactivation assay, EC50 = 0.01 μM.	23502212
L6	Function assay		24 hrs	Induction of glucose uptake in rat L6 cells pulsed with C14-deoxy glucose after 24 hrs in presence of insulin, EC50 = 4.49 μM.	23992862
L6	Function assay		16 hrs	Increase in 2-[3H]-deoxyglucose uptake in rat L6 cells after 16 hrs by scintillation counting analysis, IC50 = 4.8 μM.	24813738
HEK293	Function assay	10 uM	24 hrs	Transactivation of PPAR-gamma (unknown origin) expressed in HEK293 cells at 10 uM after 24 hrs by luciferase reporter gene assay	24890090
HEK293	Function assay		24 hrs	Agonist activity at mouse PPARgamma expressed in HEK293 cells co-expressing with Gal4 reporter vector after 24 hrs by dual-luciferase reporter assay, EC50 = 0.03 μM.	24955889
DU145	Cytotoxicity assay		48 hrs	Cytotoxicity against human DU145 cells assessed as growth inhibition after 48 hrs by MTT assay, IC50 = 16 μM.	24996143
PC3	Cytotoxicity assay		48 hrs	Cytotoxicity against human PC3 cells assessed as growth inhibition after 48 hrs by MTT assay, IC50 = 20.3 μM.	24996143
MDA-MB-231	Growth inhibition assay		24 hrs	Growth inhibition of human MDA-MB-231 cells after 24 hrs by MTT assay, IC50 = 5.23 μM.	25278236
HEK293	Function assay			Agonist activity at human PPARgamma expressed in HEK293 cells by luciferase reporter gene assay, EC50 = 0.01 μM.	25305688
HepG2	Function assay		20 hrs	Transactivation of PPAR transfected in human HepG2 cells after 20 hrs by PPAR-luciferase assay, EC50 = 1.6 μM.	25437304
HEK293	Function assay		24 hrs	Transactivation of PPARgamma (unknown origin) expressed in HEK293 cells incubated for 24 hrs by luciferase reporter gene assay	25442322
HepG2	Function assay			Agonist activity at human GAL4-PPARgamma ligand binding domain expressed in human HepG2 cells by luciferase reporter gene assay, EC50 = 0.039 μM.	25462281
HepG2	Function assay		20 hrs	Agonist activity at GAL4-DNA binding domain fused human PPARgamma ligand binding domain expressed in human HepG2 cells assessed as receptor transactivation incubated for 20 hrs by luciferase reporter gene assay, EC50 = 0.04 μM.	25497132
HepaR	Function assay	1 uM	1 day	Agonist activity at PPARgamma in human HepaR cells assessed as increase in FABP1 gene expression at 1 uM incubated for 1 day by quantitative PCR method relative to untreated control	25497132
HepaR	Function assay	1 uM	1 day	Agonist activity at PPARgamma in human HepaR cells assessed as increase in ANGPTL4 gene expression at 1 uM incubated for 1 day by quantitative PCR method relative to untreated control	25497132
HepaR	Function assay	1 uM	1 day	Agonist activity at PPARgamma in human HepaR cells assessed as increase in HMGCS2 gene expression at 1 uM incubated for 1 day by quantitative PCR method relative to untreated control	25497132
C2C12	Function assay	30 uM	2 hrs	Induction of 2-deoxy-[3H]-glucose uptake in mouse C2C12 cells at 30 uM after 2 hrs by liquid scintillation counting analysis	25835537
MCF7	Function assay		16 hrs	Agonist activity at human PPARgamma transfected in human MCF7 cells after 16 hrs by luciferase reporter gene assay, EC50 = 0.087 μM.	26226490
HEK293	Function assay	10 uM	24 hrs	Agonist activity at PPARgamma (unknown origin) expressed in HEK293 cells assessed as receptor transactivation at 10 uM incubated for 24 hrs by luciferase reporter gene assay	26384286
3T3L1	Function assay	2 uM		Transactivation of PPARgamma in mouse 3T3L1 cells assessed as adipocyte differentiation by measuring lipid accumulation at 2 uM by Oil Red O staining-based assay	26595749
3T3L1	Function assay	2 uM		Transactivation of PPARgamma in mouse 3T3L1 cells assessed as increase in FABP4 expression at 2 uM by qPCR method	26595749
3T3L1	Function assay	2 uM		Transactivation of PPARgamma in mouse 3T3L1 cells assessed as increase in GTUT4 expression at 2 uM by qPCR method	26595749
3T3L1	Function assay	2 uM		Transactivation of PPARgamma in mouse 3T3L1 cells assessed as increase in adiponectin expression at 2 uM by qPCR method	26595749
3T3L1	Function assay	2 uM		Transactivation of PPARgamma in mouse 3T3L1 cells assessed as increase in LPL expression at 2 uM by qPCR method	26595749
HEK293	Function assay	1 uM	24 hrs	Agonist activity at PPAR gamma (unknown origin) transfected in HEK293 cells at 1 uM after 24 hrs by dual-luciferase reporter gene assay	26988304
C2C12	Function assay	20 uM	4 hrs	Transactivation of PPARgamma in mouse C2C12 cells assessed as increase in GLUT-4 mediated 2-NBDG uptake at 20 uM at 4 hrs by fluorescence assay	27100993
HEK293	Function assay		24 hrs	Agonist activity at GAL4-tagged human PPARgamma ligand binding domain chimeric receptor expressed in HEK293 cells after 24 hrs by luciferase reporter gene assay, EC50 = 0.26 μM.	27591006
HepG2	Function assay		20 hrs	Transactivation of GAL4-fused human PPARgamma LBD expressed in human HepG2 cells after 20 hrs by luciferase reporter gene assay, EC50 = 0.04 μM.	28076827
HT-29	Function assay	10 uM	24 hrs	Agonist activity at PPARgamma in human HT-29 cells harboring APC mutant assessed as inhibition of Wnt/beta-catenin signaling pathway by measuring decrease in CyclinD1 level at 10 uM treated for 24 hrs by Western blot method	28076827
COS7	Function assay		24 hrs	Transactivation of human Gal4-fused PPARgamma LBD expressed in African green monkey COS7 cells after 24 hrs by luciferase reporter gene assay, EC50 = 0.004 μM.	28609708
COS7	Function assay		24 hrs	Transactivation of human Gal4-fused PPARalpha LBD expressed in African green monkey COS7 cells after 24 hrs by luciferase reporter gene assay, EC50 = 10 μM.	28609708
HEK293	Function assay		18 hrs	Agonist activity at GAL4-fused PPARgamma LBD (unknown origin) expressed in HEK293 cells assessed as receptor transactivation after 18 hrs by dual luciferase reporter gene assay, EC50 = 0.04 μM.	28667876
Ac2F	Function assay	5 uM	6 hrs	Agonist activity at full length human flag-tagged PPARgamma1 LBD expressed in rat Ac2F cells coexpressing PPRE-X3-TK at 5 uM after 6 hrs by one-glo luciferase reporter gene assay	29389121
SK-N-MC	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells	29435139
3T3-L1	Function assay	1 uM	15 days	Agonist activity at PPARgamma in mouse 3T3-L1 cells assessed as increase in CD36 mRNA expression at 1 uM after 15 days by quantitative real-time PCR method	29878767
3T3-L1	Function assay	1 uM	15 days	Agonist activity at PPARgamma in mouse 3T3-L1 cells assessed as induction of adipocyte differentiation at 1 uM after 15 days by Oil Red O staining-based assay	29878767
3T3-L1	Function assay	1 uM	15 days	Agonist activity at PPARgamma in mouse 3T3-L1 cells assessed as increase in CPT1A mRNA expression at 1 uM after 15 days by quantitative real-time PCR method	29878767
HepG2	Function assay		20 hrs	Transactivation of GAL4-tagged human PPARgamma LBD expressed in human HepG2 cells after 20 hrs by luciferase reporter gene assay, EC50 = 0.039 μM.	30199253
3T3L1	Function assay	5 uM		Induction of lipid accumulation in mouse 3T3L1 cells at 5 uM by Oil Red O staining-based assay	30199253
3T3L1	Function assay	2 uM		Induction of lipid accumulation in mouse 3T3L1 cells at 2 uM by Oil Red O staining-based assay	30199253
HepG2	Function assay	>100 nM	20 hrs	Transactivation of GAL4-tagged human PPARgamma LBD expressed in human HepG2 cells at >100 nM after 20 hrs in presence of 5 uM PPARgamma antagonist GW9662 by luciferase reporter gene assay	30199253
COS7	Function assay		24 hrs	Agonist activity at recombinant human GAL4-DBD fused PPARgamma LBD expressed in COS7 cells after 24 hrs by luciferase reporter gene assay, EC50 = 0.396 μM.	30220602
COS7	Function assay		24 hrs	Agonist activity at recombinant human GAL4-DBD fused PPARgamma LBD expressed in COS7 cells after 24 hrs by luciferase reporter gene assay, EC50 = 0.396 μM.	30241907
HEK293	Function assay		18 hrs	Agonist activity at human GAL4 fused PPARgamma-LBD expressed in HEK293 cells after 18 hrs by luciferase reporter gene assay, EC50 = 0.12 μM.	30296685
HEL 293H	Function assay		16 hrs	Transactivation of GAL4-DBD fused human PPARgamma ligand binding domain expressed in UAS-bla HEL 293H cells preincubated for 16 hrs followed by FRET substrate addition and measured after 2 hrs by TR-FRET assay, EC50 = 0.008 μM.	30429097
HEK293	Function assay		18 hrs	Transactivation of human PPARgamma expressed in HEK293 cells incubated for 18 hrs by dual luciferase reporter gene assay, EC50 = 0.039 μM.	ChEMBL
CV-1	Function assay			Tested for transactivation of human PPAR gamma-Gal4 chimera in CV-1 cells, EC50 = 0.05 μM.	ChEMBL
3T3L1	Function assay		7 days	Upregulation of FAS protein expression in differentiated mouse 3T3L1 cells after 7 days by western blot analysis	ChEMBL
3T3L1	Function assay		7 days	Upregulation of aP2 protein expression in differentiated mouse 3T3L1 cells after 7 days by western blot analysis	ChEMBL
3T3L1	Function assay		24 hrs	Inhibition of chronic insulin-stimulated insulin resistance in differentiated mouse 3T3L1 cells assessed as 2-deoxy-D-[3H]-glucose uptake after 24 hrs by scintillation counting analysis	ChEMBL
3T3L1	Function assay	10 uM	24 hrs	Induction of insulin-stimulated 2-deoxy-D-[3H]-glucose uptake in differentiated mouse 3T3L1 cells at 10 uM after 24 hrs by scintillation counting analysis	ChEMBL
3T3L1	Function assay	2 uM	14 days	Agonist activity at PPAR in mouse 3T3L1 cells assessed as increase in adipocyte differentiation at 2 uM after 14 days by Oil Red O staining method	ChEMBL
U2OS	Function assay	10 uM	24 hrs	Activation of PPARG (unknown origin) expressed in human U2OS cells at 10 uM incubated for 24 hrs by luciferase reporter gene assay	ChEMBL
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Informazioni chimiche, conservazione e stabilità

Peso molecolare	357.43	Formula	C₁₈H₁₉N₃O₃S	Conservazione (Dalla data di ricezione)	3 anni-20°Cpolvere
N. CAS	122320-73-4	Scarica SDF		Conservazione delle soluzioni stock	1 anno-80°Cin solvente 1 mese-20°Cin solvente
Sinonimi	BRL 49653			Smiles	CN(CCOC1=CC=C(C=C1)CC2C(=O)NC(=O)S2)C3=CC=CC=N3

Solubilità

In vitro
Lotto:

DMSO : 71 mg/mL (198.64 mM)
(Il DMSO contaminato da umidità può ridurre la solubilità. Utilizzare DMSO fresco e anidro.)

Water : Insoluble

Ethanol : Insoluble

Calcolatore di Molarità

Massa	Concentrazione	Volume	Peso molecolare
=	×	×

Calcolatore di Diluizione Calcolatore del Peso Molecolare

In vivo Lotto:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	4%DMSO 1 30%PEG300 2 5%Tween80 3 61%ddH2O Validato dai laboratori Selleck. Se necessiti di modifiche a questa formulazione, contatta il nostro team di vendita per test personalizzati.	5.000mg/ml (13.99mM)	Taking the 1 mL working solution as an example, add 40 μL of 125 mg/ml clarified DMSO stock solution to 300 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify it; then continue to add 610 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

Calcolatore di formulazione in vivo (Soluzione chiara)

Passo 1: Inserire le informazioni di seguito (Consigliato: Un animale aggiuntivo per tenere conto della perdita durante lesperimento)

Dosaggio: mg/kg Peso medio degli animali: g Volume di dosaggio per animale:μL Numero di animali:

Passo 2: Inserire la formulazione in vivo (Questo è solo il calcolatore, non la formulazione. Contattateci prima se non cè una formulazione in vivo nella sezione Solubilità.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Risultati del calcolo:

Concentrazione di lavoro: mg/ml;

Metodo per preparare il liquido master di DMSO: mg farmaco predissolto in μL DMSO ( Concentrazione del liquido master mg/mL, Vi preghiamo di contattarci prima se la concentrazione supera la solubilità del DMSO del lotto del farmaco. )

Metodo per preparare la formulazione in vivo: Prendere μL DMSO liquido master, quindi aggiungereμL PEG300, mescolare e chiarire, quindi aggiungereμL Tween 80, mescolare e chiarire, quindi aggiungere μL ddH₂O, mescolare e chiarire.

Metodo per preparare la formulazione in vivo: Prendere μL DMSO liquido master, quindi aggiungere μL Olio di mais, mescolare e chiarire.

Nota: 1. Si prega di assicurarsi che il liquido sia limpido prima di aggiungere il solvente successivo.
2. Assicurarsi di aggiungere il/i solvente/i in ordine. È necessario assicurarsi che la soluzione ottenuta, nellaggiunta precedente, sia una soluzione limpida prima di procedere allaggiunta del solvente successivo. Metodi fisici come il vortex, gli ultrasuoni o il bagno dacqua calda possono essere utilizzati per facilitare la dissoluzione.

Meccanismo dazione

Targets/IC₅₀/Ki	PPAR (Cell-free assay) TRPC Ferroptosis
In vitro	La Rosiglitazone aumenta marcatamente la fosforilazione della treonina 172 all'interno della subunità α di AMPK, con un aumento del rapporto AMP:ATP. È stato riportato che questo composto diminuisce la sintesi del colesterolo in diverse linee cellulari in modo indipendente dal recettore γ attivato dai proliferatori perossisomiali. Attiva i complessi AMPK contenenti sia α1 che α2, e ciò porta a un marcato aumento della fosforilazione dell'acetil-CoA carbossilasi. Questa sostanza chimica attiva PPAR-gamma2 che agisce come un inibitore dominante dell'osteoblastogenesi nel midollo osseo murino in vitro. Aumenta la secrezione di adiponectina dalle cellule omentali fino a 2.3 volte di più, mentre la secrezione dalle cellule adipose sottocutanee non è influenzata. Questo composto modifica le caratteristiche morfologiche e i profili proteici dei mitocondri negli adipociti 3T3-L1.
In vivo	La somministrazione di Rosiglitazone provoca una significativa perdita ossea, inclusa una diminuzione del volume osseo, della larghezza trabecolare e del numero di trabecole e un aumento della spaziatura trabecolare. Questo composto porta anche a una diminuzione del tasso di formazione ossea, con un contemporaneo aumento del contenuto di grasso nel midollo osseo. Diminuisce l'espressione dei geni specifici degli osteoblasti Runx2/Cbfa1, Dlx5 e collagene alfa1(I), mentre l'espressione della proteina legante gli acidi grassi aP2, specifica degli adipociti, è aumentata. Questa sostanza chimica sovraregola i trascritti genici che codificano le proteine mitocondriali negli adipociti bianchi di topi ob/ob, accompagnato da un aumento della massa mitocondriale e cambiamenti nella struttura mitocondriale.
Riferimenti	[1] https://pubmed.ncbi.nlm.nih.gov/11994296/ [2] https://pubmed.ncbi.nlm.nih.gov/14500573/ [3] https://pubmed.ncbi.nlm.nih.gov/12466369/ [4] https://pubmed.ncbi.nlm.nih.gov/15520860/ [5] https://pubmed.ncbi.nlm.nih.gov/21406603/ [6] https://pubmed.ncbi.nlm.nih.gov/30737476/ [7] https://pubmed.ncbi.nlm.nih.gov/35131600/ [8] https://pubmed.ncbi.nlm.nih.gov/28892640/

Applicazioni

Metodi	Biomarcatori	PMID
Western blot	Cyclin D1 / CDK2 / CDK4 / Bax / Bcl-2	29725405
Immunofluorescence	PPARγ / E-cadherin	27145370
Growth inhibition assay	Cell viability	29725405

Informazioni sullo studio clinico

(dati da https://clinicaltrials.gov, aggiornato il 2024-05-22)

Numero NCT	Reclutamento	Condizioni	Sponsor/Collaboratori	Data di inizio	Fasi
NCT02737709	Terminated	Non-small Cell Lung Cancer	Sun Yat-sen University	March 2016	Phase 2
NCT01402076	Completed	Healthy Volunteers	Vanda Pharmaceuticals	August 2011	Phase 1
NCT01100619	Completed	Papillary Thyroid Cancer\|Follicular Thyroid Cancer\|Huerthle Cell Thyroid Cancer\|Renal Cell Carcinoma	Exelixis	April 2010	Phase 1
NCT01415128	Completed	Erectile Dysfunction	VIVUS LLC	April 2010	Phase 1
NCT01376063	Completed	Healthy Adult Subjects	FibroGen	March 2010	Phase 1

Supporto tecnico

Istruzioni per la manipolazione

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