Home Metabolism agonista Calcitriol (1,25-Dihydroxyvitamin D3)

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Calcitriol (1,25-Dihydroxyvitamin D3) Agonista del RVD

N. Cat.S1466

Il Calcitriol è un attivatore/agonista non selettivo del recettore della vitamina D (VDRA), che esibisce un'affinità di legame al recettore della vitamina D (VDR) 10 volte superiore (IC50=0,4 nM) rispetto al VDRA selettivo paricalcitol. Le soluzioni sono instabili e devono essere preparate al momento.
Calcitriol (1,25-Dihydroxyvitamin D3) agonista Chemical Structure

Struttura chimica

Peso molecolare: 416.64

Vai a

Controllo Qualità

Lotto: Purezza: 99.96%
99.96

Coltura cellulare, trattamento e concentrazione di lavoro

Linee cellulari Tipo di saggio Concentrazione Tempo di incubazione Formulazione Descrizione dellattività PMID
human HCT116 Cytotoxic assay 120 h Cytotoxicity against human HCT116 assessed as decrease in cell count after 120 hrs, IC50=1e-05 μM 22926068
HOS Function assay Activity at human VDR expressed in human HOS cells transfected with pGL3-hOc, pCDNA-hVDR and phRL-TK assessed as assessed as transcriptional activation measured 24 hrs post infection by luciferase reporter gene assay, EC50 = 0.00001 μM. 21889334
SK-MEL-188 Growth inhibition assay 48 hrs Growth inhibition of human SK-MEL-188 cells measured after 48 hrs by MTS/PMS assay, IC50 = 0.00001 μM. 27070779
osteosarcoma cells Function assay Effect on VDR transcriptional activity in human osteosarcoma cells, EC50 = 0.0000106 μM. 18054230
HOS/SF Function assay 24 hrs Transactivation of VDR-mediated osteocalcin promoter in human HOS/SF cells after 24 hrs by luciferase reporter gene assay, EC50 = 0.000026 μM. 24900728
LM05e Antiproliferative assay 72 hrs Antiproliferative activity against mouse LM05e cells assessed as decrease in cell number after 72 hrs by WST assay, IC50 = 0.00003 μM. 24900339
HEK293 Function assay Transrepression of VP16-tagged VDR (unknown origin) expressed in HEK293 cells harboring pCMX-GAL4-NCoR and MH100(UAS) X 4tk-LUC reporter plasmid assessed as increase in NCoR recruitment by beta-galactosidase reporter gene based mammalian two-hybrid assay, IC50 = 0.00005 μM. 29989817
HEK293 Function assay Transactivation of VP16-tagged VDR (unknown origin) expressed in HEK293 cells harboring pCMX-GAL4-RXRalpha and MH100(UAS) X 4tk-LUC reporter plasmid assessed as increase in interaction with RXRalpha by beta-galactosidase reporter gene based mammalian two-, EC50 = 0.00007 μM. 29989817
HEK293T Function assay Agonist activity at GAL4 DNA-binding domain fused VDR (unknown origin) ligand binding domain expressed in UAS-bla HEK 293T cells assessed as beta-lactamase transcriptional activation by FRET-based GeneBLAzer assay, IC50 = 0.0000953 μM. 30144697
HEK293 Function assay Agonist activity at VDR (unknown origin) expressed in HEK293 cells cotransfected with NCoR assessed as decrease in NCoR recruitment by two-hybrid assay, IC50 = 0.0001 μM. 26613420
HEK293 Function assay 16 to 24 hrs Agonist activity at VDR in human HEK293 cells assessed as transcriptional activity after 16 to 24 hrs by luciferase reporter gene assay, EC50 = 0.00012 μM. 26613420
ROS 17/2.8 Function assay 16 hrs Activity at VDR in rat ROS 17/2.8 cells assessed as transcriptional activation of 24-hydroxylase gene promoter after 16 hrs by luciferase reporter gene assay, EC50 = 0.0002 μM. 19167893
osteosarcoma cells Function assay Activity at VDR in rat osteosarcoma cells assessed as 24-hydroxylase transcription by reporter gene assay, EC50 = 0.0002 μM. 17960924
ROS 17/2.8 Function assay 16 hrs Activity at rat recombinant full length VDR expressed in rat ROS 17/2.8 cells transfected with 24-hydroxylase gene promoter assessed as transcriptional activation after 16 hrs by luciferase reporter gene assay, EC50 = 0.0002 μM. 18722130
ROS 17/2.8 Function assay 16 hrs Activity at rat recombinant full length VDR expressed in rat ROS 17/2.8 cells transfected with 24-hydroxylase gene promoter assessed as transcriptional activation after 16 hrs by luciferase reporter gene assay, Ki = 0.0002 μM. 21105677
ROS 17/2.8 Function assay 16 hrs Agonist activity at rat VDR in ROS 17/2.8 cells transfected with Cyp24a1 reporter plasmid assessed as increase in Cyp24a1 transcription after 16 hrs by luciferase reporter gene assay, EC50 = 0.0002 μM. 22018918
osteosarcoma cells Function assay Induction of VDR-mediated 24-hydroxylase transcription in rat osteosarcoma cells by luciferase reporter gene assay, ED50 = 0.0002 μM. 21902235
osteosarcoma cells Function assay Transactivation of VDR in rat osteosarcoma cells assessed as 24-hydroxylase transcriptional activity by luciferase reporter gene assay, ED50 = 0.0002 μM. 26630444
osteosarcoma cells Function assay 16 hrs Inhibition of VDR-induced 24-hydroxylase transcription in rat osteosarcoma cells after 16 hrs by luciferase reporter gene assay, ED50 = 0.0002 μM. 22490010
osteosarcoma cells Function assay Activity at VDR in rat osteosarcoma cells assessed as induction of 24-hydroxylase reporter gene transcription by luciferase reporter gene assay, EC50 = 0.0003 μM. 19819702
HuH7 Function assay 24 hrs Agonist activity at VDR expressed in human HuH7 cells after 24 hrs by pDR3-luciferase reporter gene assay, EC50 = 0.0003 μM. 27145071
ROS 17/2.8 Function assay Vitamin D3 receptor-mediated transcriptional potency in rat osteosarcoma ROS 17/2.8 cells, ED50 = 0.00035 μM. 10479276
ROS 17/2.8 Function assay In vitro vitamin D receptor (VDR)-mediated transcriptional potency in rat osteosarcoma ROS 17/2.8 cells, ED50 = 0.00036 μM. 11000014
ROS 17/2.8 Function assay In vitro vitamin D receptor-mediated antiproliferative activity in rat osteosarcoma ROS 17/2.8 cells, ED50 = 0.0004 μM. 11931627
COS7 Function assay Induction of transactivation of human VDR responsive gene in COS7 cells by rat osteopontin luciferase reporter gene assay, EC50 = 0.0005 μM. 17298045
COS7 Function assay 24 hrs Agonist activity at human VDR in COS7 cells assessed as induction of transcriptional transactivation after 24 hrs by mouse osteopontin luciferase reporter gene assay, EC50 = 0.0005 μM. 17904370
SVEC Antiproliferative assay 72 hrs Antiproliferative activity against mouse SVEC cells assessed as decrease in cell number after 72 hrs by WST assay, IC50 = 0.00052 μM. 24900339
osteosarcoma cells Function assay Effect on VDR transcriptional activity in human osteosarcoma cells in presence of 5% fetal calf serum, EC50 = 0.000555 μM. 18054230
HEK293 Function assay Agonist activity at VDR (unknown origin) expressed in HEK293 cells cotransfected with RXRalpha assessed as RXRalpha recruitment by two-hybrid assay, EC50 = 0.0006 μM. 26613420
CV1 Function assay Activity on human VDR-mediated transcription of osteocalcin VDRE fused to thymidine kinase promoter/growth hormone reporter gene in CV1 cells, ED50 = 0.0007 μM. 17149880
NHEK Antiproliferative assay 24 hrs Antiproliferative activity against NHEK cells incubated for 24 hrs by [3H]thymidine incorporation assay, EC50 = 0.000728 μM. 22404326
COS1 Function assay Displacement of 1-alpha, 25-(OH)[3H]D3 from human VDR expressed in COS1 cells, IC50 = 0.0008 μM. 17924616
HEK293 Function assay 24 hrs Agonist activity at human VDR in HEK293 cells assessed as induction of transcriptional transactivation after 24 hrs by mouse osteopontin luciferase reporter gene assay, EC50 = 0.001 μM. 17904370
HL60 Function assay Induction of human HL60 differentiation assessed as cells reducing nitro blue tetrazolium, ED50 = 0.001 μM. 21902235
HeLa Function assay 16 hrs Transactivation of GAL4-fused VDR ligand binding domain expressed in human HeLa cells after 16 hrs by luciferase reporter gene assay, EC50 = 0.001 μM. 22957834
T47D Antiproliferative assay 72 hrs Antiproliferative activity against human T47D cells assessed as decrease in cell number after 72 hrs by WST assay, IC50 = 0.0013 μM. 24900339
ROS 17/2.8 Function assay Activity at human recombinant VDR in ROS 17/2.8 cells transfected with growth hormone fusion gene VDRE assessed as growth hormone level by transcriptional assay, ED50 = 0.0015 μM. 17924616
HEK293 Function assay 24 hrs Transactivation of recombinant human VDR/RXRalpha expressed in HEK293 cells after 24 hrs by Dual-luciferase reporter gene assay, EC50 = 0.00158 μM. 30193216
MCF7 Function assay 24 hrs Agonist activity at VDR in human MCF7 cells assessed as increase in transcription of CYP24A1 gene after 24 hrs by luciferase reporter gene assay, EC50 = 0.0016 μM. 29733645
MCF10DCIS.com Antiproliferative assay 3 days Antiproliferative activity against ER positive human MCF10DCIS.com cells after 3 days by [3H]thymidine uptake assay, IC50 = 0.00175 μM. 22180837
HL60 Function assay Induction of differention of human HL60 cells into monocytes by NBT reduction assay, EC50 = 0.002 μM. 17960924
HL-60 Function assay 4 days Induction of differentiation of human HL-60 cells promyelocytes to monocytes after 4 days by NBT reduction assay, EC50 = 0.002 μM. 18722130
bone marrow cells Function assay 3 days Effect on osteoclast formation in ddY mouse bone marrow cells co cultured with primary osteoclasts after 3 days, EC50 = 0.002 μM. 18539034
HL60 Function assay 4 days Induction of differentiation of human HL60 cells promyelocytes to monocytes after 4 days by NBT reduction assay, Ki = 0.002 μM. 21105677
HeLa Function assay 18 hrs Transactivation of full length human VDR expressed in human HeLa cells assessed as increase in CYP24 transcription after 18 hrs by luciferase reporter gene assay, EC50 = 0.0025 μM. 22957834
PBMC Function assay In vitro inhibition of phytohemagglutininin-induced stimulation of human peripheral blood mononuclear cells proliferation, ED50 = 0.0027 μM. 11000014
HL60 Function assay Induction of cell differentiation of human HL60 cells to monocytes by NBT reduction assay, EC50 = 0.003 μM. 19167893
HEK293 Function assay Agonist activity at CMX-GAL4 tagged human VDR expressed in HEK293 cells assessed as increase in transcriptional activity by luciferase reporter gene assay, EC50 = 0.003 μM. 23462715
MCF7 Function assay 24 hrs Agonist activity at VDR in human MCF7 cells assessed as transcription of CYP24A1 gene after 24 hrs by luciferase reporter gene assay, EC50 = 0.00328 μM. 22989379
Caco-2 Function assay Effect on VDR transcriptional activity in human Caco-2 cells in presence of 5% fetal calf serum, EC50 = 0.00352 μM. 18054230
MCF10AT1 Antiproliferative assay 3 days Antiproliferative activity against ER positive human MCF10AT1 cells after 3 days by [3H]thymidine uptake assay, IC50 = 0.0039 μM. 22180837
Jurkat Function assay 24 hrs Activation of VDR in human Jurkat cells expressing lentiviral VDRE-luciferase vector assessed as VDRE-mediated transcriptional activity measured after 24 hrs by luciferase transcriptional reporter assay, EC50 = 0.003936 μM. 27070779
MCF7 Function assay Agonist activity at zebrafish gal4-VDR LBD expressed in human MCF7 cells by luciferase reporter gene based transactivation assay, EC50 = 0.0055 μM. 22180837
MCF10CA1a Antiproliferative assay 3 days Antiproliferative activity against ER positive human MCF10CA1a cells after 3 days by [3H]thymidine uptake assay, IC50 = 0.0062 μM. 22180837
HL60 Function assay 96 hrs Agonist activity at VDR in human HL60 cells assessed as induction of cell differentiation after 96 hrs by NBT assay, EC50 = 0.009 μM. 29518319
HL-60 Function assay 96 hrs Agonist activity at vitamin D3 receptor in human HL-60 cells assessed as induction of cell differentiation after 96 hrs by NBT dye-based microscopic analysis, EC50 = 0.009 μM. 26562542
THP1 Function assay Activation of VDR in human THP1 cells assessed as increase in 25-hydroxyvitamin D-24-hydroxylase mRNA expression by RT-PCR, EC50 = 0.01 μM. 19309155
THP1 Function assay Activation of VDR in human THP1 cells assessed as increase in cathelicidin antimicrobial peptide mRNA expression by RT-PCR, EC50 = 0.01 μM. 19309155
ROS 17/2.8 Function assay Effective dose for transcriptional activation in ROS 17/2.8 osteosarcoma cells, ED50 = 0.01 μM. 10893309
HL60 Function assay 144 hrs Induction of cell differentiation of human HL60 cells incubated for 144 hrs by Wst-1 dye based assay, IC50 = 0.05 μM. 25180926
MCF7 Antiproliferative assay 72 hrs Antiproliferative activity against human MCF7 cells after 72 hrs by [3H]thymidine incorporation assay, EC50 = 0.052 μM. 19739672
bone marrow cells Function assay 3 days Effect on osteoclast formation in ddY mouse bone marrow cells co cultured with primary osteoclasts after 3 days relative to 1-alpha, 25-(OH)2D3, EC50 = 0.1 μM. 18539034
HL-60 Function assay Inhibition of colony formation assays on HL-60 cells, ED50 = 0.13 μM. 10893309
Caco2 Function assay 24 hrs Activation of VDR in human Caco2 cells expressing lentiviral VDRE-luciferase vector assessed as VDRE-mediated transcriptional activity measured after 24 hrs by luciferase transcriptional reporter assay, EC50 = 0.2234 μM. 27070779
HaCaT Function assay 24 hrs Activation of VDR in human HaCaT cells expressing lentiviral VDRE-luciferase vector assessed as VDRE-mediated transcriptional activity measured after 24 hrs by luciferase transcriptional reporter assay, EC50 = 0.2497 μM. 27070779
HaCaT Function assay 24 hrs Transactivation of VDR in human HaCaT cells after 24 hrs by luciferase reporter gene assay, EC50 = 0.3215 μM. 26367019
MCF-7 Function assay Inhibition of colony formation assays on MCF-7 cells, ED50 = 0.38 μM. 10893309
CV1 Function assay Effect on VDR-mediated transcriptional activity in CV1 cells transfected with human recombinant VDR, ED50 = 0.4 μM. 15615534
Caco2 Function assay 24 hrs Transactivation of VDR in human Caco2 cells after 24 hrs by luciferase reporter gene assay, EC50 = 0.5152 μM. 26367019
HN12 Antiproliferative assay 72 hrs Antiproliferative activity against human HN12 cells assessed as decrease in cell number after 72 hrs by WST assay, IC50 = 0.553 μM. 24900339
L02 Antiproliferative assay 48 hrs Antiproliferative activity against human L02 cells after 48 hrs by MTT assay, IC50 = 0.67 μM. 29518319
L02 Cytotoxicity assay 48 hrs Cytotoxicity against human L02 cells after 48 hrs by MTT assay, IC50 = 0.67 μM. 26562542
Caco2 Antiproliferative assay 48 hrs Antipoliferative activity against human Caco2 cells after 48 hrs by MTT assay, IC50 = 4.4 μM. 26562542
Caco2 Antiproliferative assay 48 hrs Antiproliferative activity against human Caco2 cells after 48 hrs by MTT assay, IC50 = 4.46 μM. 29518319
MCF7 Antiproliferative assay 48 hrs Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay, IC50 = 5.59 μM. 29518319
MCF7 Antiproliferative assay 48 hrs Antipoliferative activity against human MCF7 cells after 48 hrs by MTT assay, IC50 = 5.6 μM. 26562542
MCF7 Function assay 16 hrs Binding affinity to VDR in scrambled siRNA-transfected human MCF7 cells assessed as cell growth inhibition by measuring reduction in BrdU incorporation after 16 hrs by ELISA, IC50 = 6.43 μM. 30193216
PC3 Antiproliferative assay 24 hrs Antiproliferative activity against human PC3 cells after 24 hrs by MTT assay, IC50 = 9.53 μM. 30193216
MCF7 Antiproliferative assay 24 hrs Antiproliferative activity against human MCF7 cells after 24 hrs by MTT assay, IC50 = 11.43 μM. 30193216
MCF7 Antiproliferative assay 72 hrs Antiproliferative activity against human MCF7 cells assessed as inhibition of proliferation after 72 hrs by MTT assay, IC50 = 12.5 μM. 25127149
PC3 Antiproliferative assay 48 hrs Antipoliferative activity against human PC3 cells after 48 hrs by MTT assay, IC50 = 17.2 μM. 26562542
PC3 Antiproliferative assay 48 hrs Antiproliferative activity against human PC3 cells after 48 hrs by MTT assay, IC50 = 17.25 μM. 29518319
BxPC3 Antiproliferative assay 24 hrs Antiproliferative activity against human BxPC3 cells after 24 hrs by MTT assay, IC50 = 21.07 μM. 30193216
PBMC Function assay 10 nM up to 8 hrs Activation of VDR in LPS-stimulated human PBMC cells assessed as increase in 25-hydroxyvitamin D-24-hydroxylase mRNA expression at 10 nM after upto 8 hrs by RT-PCR 19309155
THP1 Function assay Activation of VDR in human THP1 cells assessed as increase in cathelicidin antimicrobial peptide mRNA expression at EC50 upto 5 hrs by RT-PCR 19309155
NB4 Function assay 1 nM 48 hrs Induction of cell differentiation in human NB4 cells assessed as induction of induction of cell surface marker CD14 expression at 1 nM after 48 hrs 19685888
NB4 Function assay 1 nM 48 hrs Induction of cell differentiation in human NB4 cells assessed as induction of induction of cell surface marker CD11b expression at 1 nM after 48 hrs 19685888
HL60 Function assay 4 days Induction of cell differentiation in human HL60 cells after 4 days by NBT reduction assay 19193059
HL60 Function assay 10 μM Inhibition of 1,25-(OH)2D3-induced cell differentiation in human HL60 cells assessed as morphological changes at 10'-6 M by Wright-Geimsa staining 19193059
SCC4 Function assay 1 uM 5 to 10 mins Agonist activity at VDR in human SCC4 cells assessed as induction of CYP24 gene expression at 1 uM after 5 to 10 mins by RT-PCR analysis 20452225
SCC25 Function assay 10 nM Agonist activity at VDR in human SCC25 cells assessed as induction of CYP24 expression at 10 nM 20883026
SCC25 Function assay 100 nM Agonist activity at VDR in human SCC25 cells assessed as induction of TSLP expression at 100 nM 20883026
C3H10T1/2 Function assay 0.5 to 5 uM 24 hrs Inhibition of Hedgehog signaling pathway in mouse C3H10T1/2 cells assessed as down regulation of Gli1 at 0.5 to 5 uM after 24 hrs by RT-PCR analysis 22226657
HL60 Function assay 1 μM Induction of vitamin D receptor-mediated differentiation of human HL60 cells at 10'-5 M by NBT reduction method 22285943
HL60 Function assay 1 nM to 10 μM Induction of vitamin D receptor-mediated differentiation of human HL60 cells at 10'-9 to 10'-5 M by NBT reduction method 22285943
A498 Function assay 10 nM 4 hrs Induction of CYP24 mRNA expression in human A498 cells at 10'-8 M after 4 hrs by RT-PCR analysis 21392983
A498 Function assay 10 nM 16 hrs Induction of CYP24 mRNA expression in human A498 cells at 10'-8 M after 16 hrs by RT-PCR analysis 21392983
DU145 Function assay 7.5 uM 18 hrs Agonist activity at VDR-LBD in human DU145 cells assessed as CYP24A1 expression at 7.5 uM after 18 hrs by qRT-PCR method 26774929
HaCaT Function assay Inhibition of colony formation of human HaCaT cells 22404326
HCT116 Function assay 20 to 40 uM 24 hrs Agonist activity at RAR (unknown origin) expressed in human HCT116 cells co-expressing RARE at 20 to 40 uM after 24 hrs by luciferase reporter gene assay 23276449
HCT116 Function assay 20 to 40 uM 24 hrs Agonist activity at RXR (unknown origin) expressed in human HCT116 cells co-expressing RXRE at 20 to 40 uM after 24 hrs by luciferase reporter gene assay 23276449
HEK293 Function assay 100 nM 24 hrs Induction of cyp24A1 mRNA expression in HEK293 cells at 100 nM after 24 hrs by real-time PCR 24773565
HEK293 Function assay 10 nM Transactivation of human VDR D149A mutant expressed in HEK293 cells coexpressing CYP3A4 at 10 nM by dual luciferase reporter gene assay 24818857
HEK293 Function assay 10 nM Transactivation of human VDR K240A mutant expressed in HEK293 cells coexpressing CYP3A4 at 10 nM by dual luciferase reporter gene assay 24818857
MCF7 Antitumor assay 0.5 mg/kg 3 weeks Antitumor activity against human MCF7 cells xenografted in Balb/c nude mouse assessed as increase in p21 expression at 0.5 mg/kg, ip administered three times a week for three weeks starting from day 7 after tumor cell inoculation by immunohistochemical an 30193216
MCF7 Antitumor assay 0.5 mg/kg 3 weeks Antitumor activity against human MCF7 cells xenografted in Balb/c nude mouse assessed as increase in p27 expression at 0.5 mg/kg, ip administered three times a week for three weeks starting from day 7 after tumor cell inoculation by immunohistochemical an 30193216
MCF7 Antitumor assay 0.5 mg/kg 3 weeks Antitumor activity against human MCF7 cells xenografted in Balb/c nude mouse assessed as reduction in tumor growth at 0.5 mg/kg, ip administered three times a week for three weeks starting from day 7 after tumor cell inoculation 30193216
MCF7 Antitumor assay 0.5 mg/kg 3 weeks Antitumor activity against human MCF7 cells xenografted in Balb/c nude mouse assessed as increase in Bax expression at 0.5 mg/kg, ip administered three times a week for three weeks starting from day 7 after tumor cell inoculation by immunohistochemical an 30193216
C3H10T1/2 Function assay 0.5 uM 24 hrs Activation of hedgehog signaling pathway in non-targeting siRNA treated mouse C3H10T1/2 cells assessed as effect on VDR expression at 0.5 uM after 24 hrs by qPCR analysis 24730984
C3H10T1/2 Function assay 0.5 uM 24 hrs Activation of hedgehog signaling pathway in VDR-knockdown mouse C3H10T1/2 cells assessed as effect on VDR expression at 0.5 uM after 24 hrs by qPCR analysis 24730984
C3H10T1/2 Function assay 0.5 uM 24 hrs Effect on CYP24A1 RNA level in non-targeting siRNA treated mouse C3H10T1/2 cells at 0.5 uM after 24 hrs by qPCR analysis 24730984
C3H10T1/2 Function assay 0.5 uM 24 hrs Inhibition of hedgehog signaling pathway in non-targeting siRNA treated mouse C3H10T1/2 cells assessed as effect on VDR expression at 0.5 uM after 24 hrs by qPCR analysis 24730984
C3H10T1/2 Function assay 0.5 uM 24 hrs Inhibition of hedgehog signaling pathway in VDR-knockdown mouse C3H10T1/2 cells assessed as effect on VDR expression at 0.5 uM after 24 hrs by qPCR analysis 24730984
LX2 Function assay 100 nM 24 hrs Transactivation of VDR in human LX2 cells assessed as inhibition of TGFbeta1-induced COL1A1 mRNA expression at 100 nM after 24 hrs by Q-PCR analysis 30350999
ROS 17/2.8 Function assay 16 hrs Induction of VDR transcriptional activity assessed as activation of 24-hydroxylase gene expression in rat ROS 17/2.8 cells after 16 hrs by luciferase reprter assay 26574921
HL60 Function assay 30 to 1000 nM 48 hrs Induction of cell differentiation in human HL60 cells assessed as maturing morphological changes at 30 to 1000 nM after 48 hrs by Wright's-Giemsa staining-based forty microscopic view assay 25127149
SW480-ADH Function assay 100 nM 48 hrs Induction of human SW480-ADH cell differentiation assessed as formation of compact epithelioid islands of highly adherent cells at 10 '-7 M after 48 hrs by phase-contrast microscopy 22989379
SW480-ADH Function assay 10 nM 48 hrs Induction of human SW480-ADH cell differentiation assessed as formation of compact epithelioid islands of highly adherent cells at 10 '-8 M after 48 hrs by phase-contrast microscopy 22989379
MCF7 Antiproliferative assay 100 nM 48 hrs Antiproliferative activity against human MCF7 cells at 10 '-7 M after 48 hrs by MTT assay relative to untreated-control 22989379
CLL Function assay 100 nM 24 hrs Effect on CYP24A1 in human primary CLL cells assessed as increase in VDR-regulated GADD45alpha mRNA expression at 100 nM incubated for 24 hrs by quantitative RT-PCR method 25148392
CLL Function assay 100 nM 24 hrs Effect on CYP24A1 in human primary CLL cells assessed as increase in VDR-regulated CDKN1A mRNA expression at 100 nM incubated for 24 hrs by quantitative RT-PCR method 25148392
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Informazioni chimiche, conservazione e stabilità

Peso molecolare 416.64 Formula

C27H44O3

 Conservazione (Dalla data di ricezione) 1 year -80°C powder（in dark and seal）
N. CAS 32222-06-3 Scarica SDF Conservazione delle soluzioni stock Le soluzioni sono instabili. Preparare al momento o acquistare formati piccoli e preconfezionati. Riconfezionare al ricevimento.
Sinonimi RO215535, Topitriol, 1,25-Dihydroxyvitamin D3 Smiles CC(CCCC(C)(C)O)C1CCC2C1(CCCC2=CC=C3CC(CC(C3=C)O)O)C

Solubilità

In vitro
Lotto:

DMSO : 83 mg/mL (199.21 mM)
(Il DMSO contaminato da umidità può ridurre la solubilità. Utilizzare DMSO fresco e anidro.)

Ethanol : 83 mg/mL

Water : Insoluble

Calcolatore di Molarità

Massa Concentrazione Volume Peso molecolare
Calcolatore di Diluizione Calcolatore del Peso Molecolare

In vivo
Lotto:

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)

mg/kg g μL

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
vitamin D receptor
(Cell-free assay)
In vitro

Calcitriol è un potente inibitore della proliferazione linfocitaria indotta da PHA, raggiungendo il 70% di inibizione dell'incorporazione di timidina tritiata dopo 72 ore in coltura. Questo composto sopprime la produzione di interleuchina-2 (IL-2) da parte delle cellule mononucleate del sangue periferico stimolate da PHA in modo concentrazione-dipendente.

Aumenta la concentrazione di calcio intracellulare ([Ca2+]i) entro 5 s mobilizzando il calcio dal reticolo endoplasmatico e la formazione di inositolo 1,4,5-trifosfato e diacilglicerolo.

Questa sostanza chimica può inibire la proliferazione e promuovere la differenziazione delle cellule di adenocarcinoma prostatico umano. Causa una diminuzione selettiva dei livelli secreti di collagenasi di tipo IV (MMP-2 e MMP-9).

Ha attività antiproliferativa nel carcinoma a cellule squamose e nell'adenocarcinoma prostatico e migliora l'attività antitumorale degli agenti a base di platino. Questo composto, prima del paclitaxel, riduce significativamente la sopravvivenza clonogenica rispetto a uno solo dei due agenti nel carcinoma a cellule squamose murino e nelle cellule PC-3.

È un potente agente antiproliferativo in una vasta gamma di tipi di cellule maligne. I suoi effetti sono associati a un aumento dell'arresto G0/G1, all'induzione dell'apoptosi e della differenziazione, alla modulazione dell'espressione dei recettori dei fattori di crescita. Questo agente potenzia gli effetti antitumorali di molti agenti citotossici e inibisce la motilità e l'invasività delle cellule tumorali e la formazione di nuovi vasi sanguigni.

Riferimenti
  • [4] https://pubmed.ncbi.nlm.nih.gov/11309356/
  • [5] https://pubmed.ncbi.nlm.nih.gov/15225831/

Applicazioni

Metodi Biomarcatori Immagini PMID
Western blot CyclinD1 IRE1α / p-eIF2α / eIF2α / Atf4 / CHOP p-PERK / PERK FGFR1 / FGFR2 / FGFR3 / FGFR4 Wnt10b / Wnt16
S1466-WB1
28643892

Informazioni sullo studio clinico

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

Numero NCT Reclutamento Condizioni Sponsor/Collaboratori Data di inizio Fasi
NCT06169397 Enrolling by invitation
Pulmonary Sarcoidosis
Xentria Inc.
 March 1 2024 Phase 2
NCT04551170 Recruiting
Pseudohypoparathyroidism|Albright Hereditary Osteodystrophy|Pseudohypoparathyroidism Type 1a
Vanderbilt University Medical Center
 July 13 2020 Phase 2
NCT03029429 Recruiting
Pseudohypoparathyroidism|Albright Hereditary Osteodystrophy
Vanderbilt University Medical Center|Harvard University
 September 1 2018 Phase 2

Supporto tecnico

Istruzioni per la manipolazione

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