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Forskolin (Colforsin) cAMP Attivatore

Name: Forskolin (Colforsin)
Brand: Selleck Chemicals
SKU: S2449
Rating: 5 (192 reviews)

N. Cat.S2449

Forskolin (Colforsin) è un attivatore ubiquitario dell'adenilato ciclasi (AC) eucariotica in un'ampia varietà di tipi cellulari, comunemente usato per aumentare i livelli di cAMP nello studio e nella ricerca della fisiologia cellulare. La Forskolin attiva anche l'attività di PXR e FXR. La Forskolin stimola l'autophagy.

Forskolin (Colforsin) cAMP Attivatore Chemical Structure

Struttura chimica

Peso molecolare: 410.5

Vai a

Controllo Qualità (Quality Control)

Lotto: Purezza: 99.20%

99.20

Prodotti spesso usati con Forskolin (Colforsin)

SQ22536

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RepSox (E-616452)

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TTNPB (Arotinoid acid)

TTNPB and this compound along with other small molecules can convert human urine cells into neurons directly, without introducing the transcription factors or miRNAs.

EPZ004777

EPZ004777 and it are used in combination with other small molecules as cocktail in the medium for direct reprogramming of mouse fibroblasts into ciNCCs and ciCECs

Target correlati	CXCR Hedgehog/Smoothened PKA Adrenergic Receptor AChR 5-HT Receptor Histamine Receptor Dopamine Receptor Ras KRas
Altro cAMP Inibitori	ESI-09 PACAP 6-38 acetate Bithionol HJC0350 Lysipressin Acetate PACAP 1-27 Fipexide hydrochloride ST034307 HJC0197 ESI-05

Coltura cellulare, trattamento e concentrazione di lavoro
(Cell Culture, Treatment & Working Concentration)

Linee cellulari	Tipo di saggio	Concentrazione	Tempo di incubazione	Formulazione	Descrizione dell'attività	PMID
HT-29	Apoptosis Assay	40 μM	48 h	DMSO	induces changes in the phosphorylation status of PP2A targets	24997451
SW480	Apoptosis Assay	40 μM	48 h	DMSO	induces changes in the phosphorylation status of PP2A targets	24997451
HT-29	Apoptosis Assay	40 μM	48 h	DMSO	induces an activation of caspase 3/7	24997451
SW480	Apoptosis Assay	40 μM	48 h	DMSO	induces an activation of caspase 3/7	24997451
HT-29	Function Assay	40 μM	7 d	DMSO	reduces colonosphere formation capability	24997451
SW480	Function Assay	40 μM	7 d	DMSO	reduces colonosphere formation capability	24997451
HT-29	Growth Inhibition Assay	40 μM	0-72 h	DMSO	inhibits cell growth time dependently	24997451
SW480	Growth Inhibition Assay	40 μM	0-72 h	DMSO	inhibits cell growth time dependently	24997451
HT-29	Function Assay	40 μM	48 h	DMSO	activates PP2A	24997451
SW480	Function Assay	40 μM	48 h	DMSO	activates PP2A	24997451
C6	Function Assay	10 μM	20 min		increases cAMP accumulation	25069417
Huh-7	Function Assay	0-20 μM	2 h		results in a dose-dependent increase in c-Myc expression at the protein and mRNA levels	25109834
THP-1	Function Assay	1/10 μM	2 h	DMSO	suppresses MCP-1 production	25154882
BeWo	Function Assay	20 µM	48 h	DMSO	induces cell fusion	25184477
ventricular cardiomyocytes	Function Assay	0.01-10 μM			evokes an inotropic response 120±15% above basal with an EC50 of 2.2 µM	25203113
ventricular cardiomyocytes	Function Assay	0.01-10 μM			increases cAMP accumulation	25203113
MIN6	Function Assay	10 μM	3 h		increases D3 mRNA expression	25241124
L6	Function Assay	40 µM	24 h		inhibits DMH1-induced Akt activation	25247550
HEK‐CFTR	Function Assay	2–50 μM	0-12 min	DMSO	induces a dose‐dependent iodide efflux	25263207
SK-N-SH	Cell Viability Assay	10 μM	48 h		enhances SK-N-SH neuroblastoma cell viability	25266063
SK-N-AS	Function Assay	10 μM	10/30/60 min		increases levels of p-β-catenin (ser675) and induces accumulation of p-β-catenin (ser675) in (peri)nuclear regions	25266063
SK-N-AS	Function Assay	10 μM	30 min		induces phosphorylation of β-catenin (ser675), p-GSK3β (ser9) and concomitant higher levels of active, unphosphorylated, β-catenin	25266063
SK-N-AS	Function Assay	10 μM	24 h		increases the expression of cyclin D1	25266063
SK-N-AS	Function Assay	10 μM	24 h		increases the cAMP levels	25266063
SK-N-AS	Cell Viability Assay	10 μM	24/48 h		enhances time-dependently cellular viability	25266063
granulosa cells	Function Assay	10 μM	24 h		increases the levels of RGS2 promoter activity	25339105
granulosa cells	Function Assay	10 μM	24 h		increases the intensity of DNA/protein complex	25339105
granulosa cells	Function Assay	10 μM	12/24 h		increases the levels of reporter activity for the longest fragment (−854/+18RGS2.LUC)	25339105
granulosa cells	Function Assay	10 μM	12/24 h		increases the levels of RGS2 mRNA	25339105
BeWo	Function Assay	20 µM	48 h	DMSO	downregulates the level of GCM-1	25362260
BeWo	Function Assay	20 µM	48 h	DMSO	downregulates the level of TMEMF16	25362260
BeWo	Function Assay	20 µM	48 h	DMSO	increases the beta-hCG release	25362260
EM1	Function Assay	15 μM	48 h		reduces the expression of LIF or PTGS2 in CALR- or EPAC2-silenced EM1 cells	25378661
Primary bovine chondrocytes	Growth Inhibition Assay	5μM	48 h		reverses the inhibitory effect of celecoxib on proliferation in growth plate chondrocytes	25406016
RBMECs	Function Assay	5 μM	1 h		blocks the actin cytoskeleton rearrangement seen with EMAP-II treatment	25416651
RBMECs	Function Assay	5 μM	1 h		blocks the EMAP-II-induced change in MLC phosphorylation	25416651
RBMECs	Function Assay	5 μM	1 h		reverses the changes in ZO-1 distribution seen with EMAP-II treatment	25416651
RBMECs	Function Assay	5 μM	1 h		inhibits the decreased of amount of ZO-1 in MFs induced by EMAP-II	25416651
RBMECs	Function Assay	5 μM	1 h		prevents the increase in HRP flux across the BTB induced by EMAP-II	25416651
RBMECs	Function Assay	5 μM	1 h		prevents the EMAP-II-induced TEER value decrease	25416651
RBMECs	Function Assay	5 μM	1 h		blocks the activation of RhoA/ROCK induced by EMAP-II	25416651
RBMECs	Function Assay	0.05/0.5/5 μM	0.25 h		increases cAMP concentration	25416651
ThGCs	Function Assay	10 μM	3 h		inhibits the effect of H2O2 on EDN2 mRNA	25433027
ThGCs	Function Assay	10 μM	4 h		increases CoCl2-induced EDN2 gene expression	25433027
ThGCs	Function Assay	10 μM	4 h		augments HIF1A levels that were stimulated by CoCl2	25433027
LNCaP	Function Assay	10 μM	12 h	DMSO	induces a dramatic increase of CREB1 activity	25548099
BeWo	Function Assay	20 µM	48 h	DMSO	increases the adhesion of THP-1 monocytes	25566740
BeWo	Function Assay	20 µM	48 h	DMSO	increases the differentiation of BeWo cells	25566740
OCI-Ly18	Function Assay	40 μM	1 h	DMSO	induces the increment of cAMP concentrations	25576220
OCI-Ly1	Function Assay	40 μM	1 h	DMSO	induces the increment of cAMP concentrations	25576220
3T3-L1	Function Assay	2.5/5 μM	24 h		significantly decreases ATGL protein expression at all doses tested	25590597
HEK293	Function Assay	5 µM	30 min		increases cAMP levels	25591908
hADSCs	Function Assay	5 µM	30 min		increases cAMP levels	25591908
SH-SY5Y	Function Assay	10 μM	1 h		increases AGC1 mRNA level	25597433
SH-SY5Y	Function Assay	10 μM	1 h		increases LUC activity	25597433
UACC-647	Function Assay	10 μM	15 min	DMSO	increases eEF2 phosphorylation levels	25703025
UACC-647	Function Assay	10 μM	15 min	DMSO	inhibits ERK phosphorylation	25703025
UACC-647	Function Assay			DMSO	leads to a rise in cAMP levels (EC50 = 20.39 μM)	25703025
SC	Function Assay	0.5 μM	72 h		increases both Krox-20 and O1 expression in axon-related SCs but only Krox-20	25705874
SC	Function Assay	0.5 μM	24 h		mimicks the effect of cAMP analogs on O1 and MBP expression	25705874
oocytes	Function Assay	5 μM	24 h		attenuates rh-insulin action on oocyte GVBD significantly	25707854
BeWo	Function Assay	10 μM	72 h	DMSO	mediates BeWo cell differentiation	25713425
GH3	Function Assay	1 μM	6-h		induces PRL and Bmal1, but not Clock, mRNA expression	25727018
GH3	Function Assay	1 μM	6-h		attenuates the correlation between PRL and Bmal1 expression	25727018
PC12	Function Assay	25 μM	48 h		activates cAMP	25769305
BAECs	Function Assay	25 μM	24 h		enhances the activation of PPARα by 5 μM resveratrol, T4HS, or 4-PAP	25798826
GLUTag	Function Assay	10 µM	4 h		increases the pCREB levels with the IBMX	25832631
GLUTag	Function Assay	10 µM	0/2/4 h		stimulates GLP-1 secretion cotreated with IBMX	25832631
PBMC	Function Assay	50 μM	24 h		inhibits the increased secretion of TNF induced by the DPE	25866079
H295R	Function Assay	10 μM	48 h		increases steroid metabolites in the androgen, mineralo- and glucocorticoid pathways	25869556
3T3-L1 preadipocytes	Function Assay	10 μM	12 h		induces CREB phosphorylation and C/EBPβ expression	25928058
PCCL3	Function Assay	10 µM	24 h		enhances DuOx2 promoter transcription activity	25960956
SCG	Function Assay	100 μM		DMSO	reduces the excitability of SCG neurons	25962132
HEK-293	Function Assay	35 μM		DMSO	induces a conspicuous “inactivation” of the Kv2.1 current	25962132
SCG	Function Assay	20 μM		DMSO	reversibly suppresses IKV with a IC50 of 24.4 μM	25962132
PC-3	Cell Viability Assay	40 µM	24/48/72 h	DMSO	decreases cell viability time dependently	26023836
PC-3	Function Assay	40 µM	2 h	DMSO	leads to PP2A activation	26023836
SH-SY5Y	Function Assay	30 μM	30 min	DMSO	significantly increases the activation of PKA	26025137
EndoC-βH1	Function Assay	5 μM	1 h		leads to a strong cAMP increase	26028562
EndoC-βH1	Function Assay	5 μM	1 h		potentiates glucose-induced insulin secretion in the presence of glucose	26028562
RBMECs	Function Assay	5 μM	1 h		inhibits EMAP-II-induced inactivation of Rap1	26044663
AML-12	Function Assay	20 μM	3 h		induces the dephosphorylation of CRTC2	26048985
AML-12	Function Assay	20 μM	3 h		up-regulates Pgc1a, Pepck, and G6pc mRNA levels	26048985
AML-12	Function Assay	20 μM	1-8 h		increases glucose production	26048985
AML-12	Function Assay	20 μM	3 h		upregulates the phosphorylation levels at Thr-411 and Ser-493	26048985
Caco-2	Function Assay	0.1/1/10 μM	24 h		increases MRP2 protein level	26049102
Caco-2	Function Assay	0.1/1/10 μM	20 min		induces a dose-dependent increase in intracellular cAMP levels	26049102
bovine oocytes	Function Assay	100 μM	12 h		inhibits the effect of NPPA and/or NPPC to stimulate resumption of meiosis	26051611
BeWo	Function Assay	25 μM	24/48/72 h		leads to an increase in the expression of other fusion markers	26053549
Spinal cords	Function Assay	1 μM	30 min		stimulates cAMP levels	26126926
MDCK	Function Assay	10 µM	24 h	DMSO	inhibits the increased expression of FN caused by TGF-β1	26202352
MDCK	Function Assay	10 µM	24 h	DMSO	upregulates the expression of TGF-β1 and CTGF	26202352
RPMI 8226	Cell Viability Assay	0-100 μM	72 h		induces cell death dose dependently	26306624
H929	Cell Viability Assay	0-100 μM	72 h		induces cell death dose dependently	26306624
U266	Cell Viability Assay	0-100 μM	72 h		induces cell death dose dependently	26306624
OPM-2	Cell Viability Assay	0-100 μM	72 h		induces cell death dose dependently	26306624
INA-6	Cell Viability Assay	0-100 μM	72 h		induces cell death dose dependently	26306624
RBMECs	Function Assay	5 μM	1 h		blocks the Rac1 inactivation induced by EMAP-II	26358039
Mo-DCs	Function Assay	50 μM	24 h		promotes IL-23 production in the supernatant of zymosan stimulated Mo-DCs	26412948
HEK293	Function Assay	10 μM	6 h		increases phosphorylation of overexpressed KLHL3 at S433	26435498
ASK	Function assay		1 hr			2849641
Vero E6	Antiviral assay					17663539
epithelial cells	Function assay	1 uM	4, 6, and 8 days			19966789
HepG2 (DPX-2)	Function assay		24 hrs			20966043
HepG2	Function assay		24 hrs			20966043
HepG2 (DPX-2)	Function assay		24 hrs			20966043
HEK293T	Function assay	10 uM				24387325
HEK293	Function assay	10 uM	16 hrs			26435512
MCF7	Cytotoxicity assay		48 hrs			28838692
HEK293	Function assay		30 mins			30006176
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Informazioni chimiche, conservazione e stabilità (Chemical Information, Storage & Stability)

Peso molecolare	410.5	Formula	C₂₂H₃₄O₇	Conservazione (Dalla data di ricezione)	3 anni-20°Cpolvere
N. CAS	66575-29-9	Scarica SDF		Conservazione delle soluzioni stock	1 anno-80°Cin solvente 1 mese-20°Cin solvente
Sinonimi	HL 362, Coleonol			Smiles	CC(=O)OC1C(C2C(CCC(C2(C3(C1(OC(CC3=O)(C)C=C)C)O)C)O)(C)C)O

Solubilità (Solubility)

In vitro
Lotto:

DMSO : 82 mg/mL (199.75 mM)
(Il DMSO contaminato da umidità può ridurre la solubilità. Utilizzare DMSO fresco e anidro.)

Ethanol : 82 mg/mL

Water : 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.
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	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validato dai laboratori Selleck. Se necessiti di modifiche a questa formulazione, contatta il nostro team di vendita per test personalizzati.	1.050mg/ml (2.56mM)	Taking the 1 mL working solution as an example, add 50 μL 21 mg/ml clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL 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.

Calcolatore di formulazione in vivo (Soluzione chiara)

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

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 c'è 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, nell'aggiunta precedente, sia una soluzione limpida prima di procedere all'aggiunta del solvente successivo. Metodi fisici come il vortex, gli ultrasuoni o il bagno d'acqua calda possono essere utilizzati per facilitare la dissoluzione.

Meccanismo d'azione (Mechanism of Action)

Targets/IC₅₀/Ki	Adenylyl cyclase (AC) (A wide variety of cell types)
In vitro	Forskolin (Colforsin) aumenta i livelli di cAMP in preparazioni di membrane, cellule o tessuti. Non solo attiva l'Adenylyl Cyclase, ma interagisce anche con altre proteine, inclusi i trasportatori di glucosio e i canali ionici. Questo composto è in grado di promuovere l'attivazione di nove diverse isoforme transmembrana dell'Adenylyl Cyclase, sebbene con un'efficacia leggermente inferiore per l'AC9, il che potrebbe essere utilizzato per fornire un mezzo per identificare e quantificare i siti di legame ad alta affinità, cioè i complessi G-proteins (G_s)–Adenylyl Cyclase. L'attivazione di _s da parte dei GPCRs contribuisce alla generazione di cAMP stimolata da Forskolin nelle cellule a causa della potenziamento dell'attività dell'Adenylyl Cyclase da parte di _s-Forskolin. Stimola l'attività dell'adenilato ciclasi senza interagire con i recettori della superficie cellulare. Il suo potenziamento del cAMP a sua volta inibisce la degranulazione dei basofili e dei mastociti e il rilascio di istamina, abbassa la pressione sanguigna e la pressione intraoculare, inibisce l'aggregazione piastrinica, promuove la vasodilatazione, la broncodilatazione e la secrezione di ormoni tiroidei e stimola la lipolisi nelle cellule adipose. Forskolin inibisce il legame del fattore attivante le piastrine (PAF), indipendentemente dalla formazione di cAMP, il che potrebbe essere il risultato del suo effetto diretto sul PAF o tramite l'interferenza con il legame del PAF ai siti recettoriali. Sembra anche avere un effetto su diverse proteine di trasporto di membrana e inibisce il trasporto del glucosio negli eritrociti, negli adipociti, nelle piastrine e in altre cellule. Questo composto viene utilizzato per il trattamento del glaucoma.
In vivo	Forskolin (Colforsin, HL 362, Coleonol) è un attivatore ubiquitario dell'Adenylyl Cyclase (AC) eucariotica in un'ampia varietà di tipi cellulari, comunemente usato per aumentare i livelli di cAMP. Attiva anche l'attività di PXR e FXR e stimola l'Autophagy.
Riferimenti	[1] https://pubmed.ncbi.nlm.nih.gov/12825829/ [2] https://pubmed.ncbi.nlm.nih.gov/23023353/ [3] https://pubmed.ncbi.nlm.nih.gov/35286396/ [4] https://pubmed.ncbi.nlm.nih.gov/27590029/

Applicazioni (Applications)

Metodi	Biomarcatori	PMID
Western blot	p-JNK / JNK / P-p38 / p38 pS6K1 / S6K1 / pCREB / CREB c-myc / Cyclin D1 β-catenin cleaved caspase-9 / caspase-9 cleaved caspase-3 / caspase-3	20070884
Immunofluorescence	CYP17A1 / CYP21A2 Fe(II) 5hmC	25334044
Growth inhibition assay	Cell viability	30863177

Informazioni sullo studio clinico (Clinical Trial Information)

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

Numero NCT	Reclutamento	Condizioni	Sponsor/Collaboratori	Data di inizio	Fasi
NCT04254705	Withdrawn	Cystic Fibrosis	Universitaire Ziekenhuizen KU Leuven\|Vertex Pharmaceuticals Incorporated\|KU Leuven\|University of Lisbon	March 1 2020	Not Applicable
NCT02807415	Completed	Cystic Fibrosis	Hannover Medical School\|Heidelberg University\|University of Giessen	June 1 2016	--
NCT02586883	Completed	Idiopathic Dilation of the Bronchi	Assistance Publique - Hôpitaux de Paris	March 29 2016	Not Applicable
NCT03652090	Completed	Cystic Fibrosis	Institut National de la Santé Et de la Recherche Médicale France\|ABCF2	September 1 2010	--

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):