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F6886

Sigma-Aldrich

Forskolin

from Coleus forskohlii, ≥98% (HPLC), powder

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Synonym(s):
7β-Acetoxy-8,13-epoxy-1α,6β,9α-trihydroxylabd-14-en-11-one, Coleonol, Colforsin
Empirical Formula (Hill Notation):
C22H34O7
CAS Number:
66575-29-9
Molecular Weight:
410.50
Beilstein:
1692716
EC Number:
266-410-9
MDL number:
MFCD00082317
UNSPSC Code:
41106305
PubChem Substance ID:
24278035
NACRES:
NA.77

biological source

Coleus forskohlii

Quality Level

200

Assay

≥98% (HPLC)

form

powder

color

white to off-white

solubility

ethanol: soluble 50 mg/mL

SMILES string

CC(=O)O[C@H]1[C@@H](O)[C@H]2C(C)(C)CC[C@H](O)[C@]2(C)[C@@]3(O)C(=O)C[C@@](C)(O[C@]13C)C=C

InChI

1S/C22H34O7/c1-8-19(5)11-14(25)22(27)20(6)13(24)9-10-18(3,4)16(20)15(26)17(28-12(2)23)21(22,7)29-19/h8,13,15-17,24,26-27H,1,9-11H2,2-7H3/t13-,15-,16-,17-,19-,20-,21+,22-/m0/s1

InChI key

OHCQJHSOBUTRHG-KGGHGJDLSA-N

Gene Information

human ... OPRK1(4986) , SLC2A10(81031) , TNF(7124)

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General description

Forskolin, present predominantly in the root of Coleus forskohlii plant, is a potential pharmacological compound. It is used for treating hypertension, respiratory disorders and obesity. Forskolin is a diterpenoid capable of modulating adenylate cyclase enzyme and cyclic adenosine monophosphate (cAMP) levels. Engineering forskolin biosynthetic pathway caters its commercial production for pharmacological use. Forskolin has antioxidant and anti-inflammatory property and reduces hyperglycemia by stimulating insulin release. Forskolin promotes differentiation of hepatoma HepaRG cells and activates farnesoid X receptor (FXR) and pregnane X receptor(PXR).
Several studies indicate that forskolin is linked to increased lipolysis, potentially leading to increased fat and weight reduction within the body. The supplementation of forskolin is believed to potentially improve fat loss without losing muscle mass.

Application

Forskolin has been used:
  • for inducing mRNA expression in primary hepatocytes.
  • as a defatting drug in primary human hepatocytes.
  • as a medium supplement to induce differentiation of adipose-derived stem cells (ASCs).
  • in the activation of the cystic fibrosis transmembrane conductance regulator (CFTR) gene.
  • to promote the differentiation of human induced pluripotent stem cells (hiPSCs) into endothelial cells.
  • to stimulate cystic fibrosis transmembrane conductance regulator (CFTR)-mediated chloride ion secretion in differentiated airway epithelial cells derived from individuals with and without cystic fibrosis (CF).

Biochem/physiol Actions

Cell-permeable diterpenoid that possesses anti-hypertensive, positive inotropic, and adenylyl cyclase activating properties. Many of its biological effects are due to its activation of adenylyl cyclase and the resulting increase in intracellular cAMP concentration. Forskolin effects calcium currents and inhibits MAP kinase.

Features and Benefits

This compound is a featured product for Cyclic Nucleotide research. Click here to discover more featured Cyclic Nucleotide products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm.
This compound is featured on the Adenylyl cyclases page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.

Preparation Note

Forskolin is soluble in organic solvents such as ethanol, chloroform, and DMSO.

Pictograms

Exclamation mark
GHS07

Signal Word

Warning

Hazard Statements

H312

Hazard Classifications

Acute Tox. 4 Dermal

WGK

WGK 3

Personal Protective Equipment

dust mask type N95 (US), Eyeshields, Gloves

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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Establishment of pharmacokinetic parameters for the herbal drug containing forskolin
Sangeetha S, et al.
Journal of Pharmacy Research, 4(7), 2303-2306 (2011)
Effects of coleus forskohlii supplementation on body composition and hematological profiles in mildly overweight women
Henderson S, et al.
Journal of the International Society of Sports Nutrition, 2, 1-9 (2005)
Conditionally reprogrammed primary airway epithelial cells maintain morphology, lineage and disease specific functional characteristics
Martinovich KM, et al.
Scientific Reports, 7(1), 17971-17971 (2017)
Differentiation of adipose-derived stem cells into Schwann cell-like cells through intermittent induction: potential advantage of cellular transient memory function
Sun X, et al.
Stem Cell Research & Therapy, 9(1), 133-133 (2018)
Use of a high-throughput phenotypic screening strategy to identify amplifiers, a novel pharmacological class of small molecules that exhibit functional synergy with potentiators and correctors
Giuliano KA, et al.
SLAS discovery, 23(2), 111-121 (2018)
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Protocols

Forskolin-Induced Swelling Assays

A rapid in vitro assay for CFTR function, the forskolin-induced swelling protocol uses human colon organoids, which can be derived from cystic fibrosis patient tissue.

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