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Forskolin (Colforsin) cAMP activator

Name: Forskolin (Colforsin)
Brand: Selleck Chemicals
SKU: S2449
Rating: 5 (190 reviews)

Cat.nr.S2449

Forskolin (Colforsin) is een ubiquitaire activator van eukaryote adenylyl cyclase (AC) in een breed scala aan celtypen, vaak gebruikt om de niveaus van cAMP te verhogen bij de studie en het onderzoek van celfysiologie. Forskolin activeert ook PXR en FXR activiteit. Forskolin stimuleert autophagy.

Forskolin (Colforsin) cAMP activator Chemical Structure

Chemische structuur

Molecuulgewicht: 410.5

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Batch: Zuiverheid: 99.20%

99.20

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Gerelateerde doelwitten	CXCR Hedgehog/Smoothened PKA Adrenergic Receptor AChR 5-HT Receptor Histamine Receptor Dopamine Receptor Ras KRas
Overig cAMP Inhibitoren	PACAP 1-38 ESI-09 Bithionol HJC0350 PACAP 6-38 acetate Lysipressin Acetate PACAP 1-27 Fipexide hydrochloride ST034307 HJC0197

Celkweek, behandeling & werkzame concentratie

Cellijnen	Assaytype	Concentratie	Incubatietijd	Formulering	Activiteitsbeschrijving	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
Klik om meer experimentele gegevens over cellijnen te bekijken

Chemische informatie, opslag en stabiliteit

Molecuulgewicht	410.5	Formule	C₂₂H₃₄O₇	Opslag (vanaf de datum van ontvangst)	3 jaar-20°Cpoeder
CAS-nr.	66575-29-9	SDF downloaden		Opslag van stamoplossingen	1 jaar-80°Cin oplosmiddel 1 maand-20°Cin oplosmiddel
Synoniemen	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

Oplosbaarheid

In vitro
Batch:

DMSO : 82 mg/mL (199.75 mM)
(Met vocht verontreinigd DMSO kan de oplosbaarheid verminderen. Gebruik verse, watervrije DMSO.)

Ethanol : 82 mg/mL

Water : Insoluble

Molariteitscalculator

Massa	Concentratie	Volume	Molecuulgewicht
=	×	×

Verdunningscalculator Molecuulgewichtcalculator

In vivo Batch:
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 Gevalideerd door Selleck labs. Mocht u aanpassingen aan deze formulering nodig hebben, neem dan contact op met ons verkoopteam voor aangepaste tests.	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.

In vivo formulatiecalculator (heldere oplossing)

Stap 1: Voer onderstaande informatie in (Aanbevolen: een extra dier om rekening te houden met verlies tijdens het experiment)

Dosering: mg/kg Gemiddeld gewicht van dieren: g Doseervolume per dier:μL Aantal dieren:

Stap 2: Voer de in vivo formulering in (Dit is alleen de calculator, geen formulering. Neem eerst contact met ons op als er geen in vivo formulering is in de sectie oplosbaarheid.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Berekeningsresultaten:

Werkconcentratie: mg/ml;

Methode voor het bereiden van DMSO-moedervloeistof: mg geneesmiddel vooropgelost in μL DMSO ( Concentratie moedervloeistof mg/mL, Neem eerst contact met ons op als de concentratie de DMSO-oplosbaarheid van de batch van het geneesmiddel overschrijdt. )

Methode voor het bereiden van in vivo formulering: Neem μL DMSO moedervloeistof, voeg daarna toeμL PEG300, mengen en verhelderen, daarna toevoegenμL Tween 80, mengen en verhelderen, daarna toevoegen μL ddH₂O, mengen en verhelderen.

Methode voor het bereiden van in vivo formulering: Neem μL DMSO moedervloeistof, voeg daarna toe μL Maïsolie, mengen en verhelderen.

Opmerking: 1. Zorg ervoor dat de vloeistof helder is voordat u het volgende oplosmiddel toevoegt.
2. Zorg ervoor dat u het/de oplosmiddel(en) in de juiste volgorde toevoegt. U moet ervoor zorgen dat de verkregen oplossing, bij de vorige toevoeging, een heldere oplossing is voordat u verdergaat met het toevoegen van het volgende oplosmiddel. Fysieke methoden zoals vortexen, ultrasoon of een warmwaterbad kunnen worden gebruikt om het oplossen te bevorderen.

Werkingsmechanisme

Targets/IC₅₀/Ki	Adenylyl cyclase (AC) (A wide variety of cell types)
In vitro	Forskolin (Colforsin) verhoogt cAMP-niveaus in preparaten van membranen, cellen of weefsels. Het activeert niet alleen Adenylyl Cyclase, maar interageert ook met bepaalde andere eiwitten, waaronder glucosetransporters en ionkanalen. Deze verbinding is in staat om de activering van negen verschillende transmembraan-isoformen van Adenylyl Cyclase te bevorderen, zij het met iets minder werkzaamheid voor AC9, wat gebruikt zou kunnen worden om een middel te verschaffen om hoge-affiniteitsbindingsplaatsen te identificeren en kwantificeren, d.w.z. G-proteins (G_s)–Adenylyl Cyclase-complexen. Activering van _s door GPCRs draagt bij aan Forskolin-gestimuleerde cAMP-generatie in cellen vanwege _s-Forskolin-potentiëring van Adenylyl Cyclase-activiteit. Het stimuleert adenylaatcyclase-activiteit zonder interactie met celoppervlakreceptoren. De potentiëring van cAMP remt op zijn beurt de degranulatie van basofielen en mestcellen en de afgifte van histamine, verlaagt de bloeddruk en intraoculaire druk, remt bloedplaatjesaggregatie, bevordert vaatverwijding, bronchusverwijding en schildklierhormoonsecretie, en stimuleert lipolyse in vetcellen. Forskolin remt de binding van bloedplaatjesactiverende factor (PAF), onafhankelijk van cAMP-vorming, wat een gevolg kan zijn van het directe effect ervan op PAF of via interferentie met PAF-binding aan receptoren. Het lijkt ook een effect te hebben op verschillende membraantransporteiwitten en remt glucosetransport in erytrocyten, adipocyten, bloedplaatjes en andere cellen. Deze verbinding wordt gebruikt om glaucoom te behandelen.
In vivo	Forskolin (Colforsin, HL 362, Coleonol) is een ubiquitaire activator van eukaryote Adenylyl Cyclase (AC) in een breed scala aan celtypen, vaak gebruikt om de cAMP-niveaus te verhogen. Het activeert ook PXR- en FXR-activiteit en stimuleert Autophagy.
Referenties	[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/

Toepassingen

Methoden	Biomarkers	PMID
Western blot	cleaved caspase-3 / caspase-3 cleaved caspase-9 / caspase-9 β-catenin c-myc / Cyclin D1 pS6K1 / S6K1 / pCREB / CREB p-JNK / JNK / P-p38 / p38	30863177
Immunofluorescence	5hmC Fe(II) CYP17A1 / CYP21A2	29239726
Growth inhibition assay	Cell viability	30863177

Informatie over klinische proeven

(gegevens van https://clinicaltrials.gov, bijgewerkt op 2024-05-22)

NCT-nummer	Werving	Aandoeningen	Sponsor/medewerkers	Startdatum	Fasen
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	--

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