Synonym
Coleonol; Forskolin; Colforsin; HL 362; HL362; HL-362; L 75-1362B; L-75-1362B; L75-1362B; NSC 357088; NSC357088; NSC-357088; NSC 375489; NSC375489; NSC-375489;
IUPAC/Chemical Name
(3R,4aR,5S,6S,6aS,10S,10aR,10bS)-6,10,10b-trihydroxy-3,4a,7,7,10a-pentamethyl-1-oxo-3-vinyldodecahydro-1H-benzo[f]chromen-5-yl acetate
InChi Key
OHCQJHSOBUTRHG-KGGHGJDLSA-N
InChi Code
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
SMILES Code
C[C@@](C1)(C=C)O[C@]2(C)[C@@H](OC(C)=O)[C@@H](O)[C@@]3([H])C(C)(C)CC[C@H](O)[C@]3(C)[C@@]2(O)C1=O
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
Biological target:
Forskolin is an adenylate cyclase activator with an IC50 of 41 nM and an EC50 of 0.5 μM for type I adenylyl cyclase.
In vitro activity:
This study suggests that forskolin increases unliganded and liganded ERα and ERβ ubiquitination but uncouples them from proteasome-mediated degradation, regardless of their transcriptional responses to forskolin. Forskolin stimulated ERα-, but not ERβ-dependent transcription. In GH3 cells, transfected ERα mutants and ERβ were protected from degradation by forskolin. Ubiquitination of ERα and ERβ was increased by forskolin.
Reference: Int J Endocrinol. 2022 May 9;2022:7690166. https://pubmed.ncbi.nlm.nih.gov/35586275/
In vivo activity:
This study demonstrates that forskolin can regulate glucose metabolism and reduce fat cell diameter and of high-fat diet-fed mice and inhibit the adipocyte differentiation of murine mesenchymal stem cells. Forskolin administration linearly decreased blood glucose levels and the gonadal adipocyte diameter of high-fat diet-fed mice.
Reference: Animals (Basel). 2021 Mar 1;11(3):645. https://pubmed.ncbi.nlm.nih.gov/33804418/
|
Solvent |
mg/mL |
mM |
| Solubility |
| DMSO |
82.0 |
199.76 |
| Ethanol |
82.0 |
199.76 |
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.
Preparing Stock Solutions
The following data is based on the
product
molecular weight
410.51
Batch specific molecular weights may vary
from batch to batch
due to the degree of hydration, which will
affect the solvent
volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass |
1 mg |
5 mg |
10 mg |
| 1 mM |
1.15 mL |
5.76 mL |
11.51 mL |
| 5 mM |
0.23 mL |
1.15 mL |
2.3 mL |
| 10 mM |
0.12 mL |
0.58 mL |
1.15 mL |
| 50 mM |
0.02 mL |
0.12 mL |
0.23 mL |
Formulation protocol:
1. Tsai HW, Lin VY, Shupnik MA. Forskolin Stimulates Estrogen Receptor (ER) α Transcriptional Activity and Protects ER from Degradation by Distinct Mechanisms. Int J Endocrinol. 2022 May 9;2022:7690166. doi: 10.1155/2022/7690166. PMID: 35586275; PMCID: PMC9110234.
2. Yang P, Jiang PW, Li C, Gao MX, Sun YS, Zhang DY, Du WQ, Zhao J, Shi ST, Li Y, Yang T, Cheng L, Li MH. Cdc25C/cdc2/cyclin B, raf/MEK/ERK and PERK/eIF2α/CHOP pathways are involved in forskolin-induced growth inhibition of MM.1S cells by G2/M arrest and mitochondrion-dependent apoptosis. Cell Cycle. 2021 Nov;20(22):2402-2412. doi: 10.1080/15384101.2021.1983280. Epub 2021 Oct 4. PMID: 34606419; PMCID: PMC8794531.
3. Dagda RK, Dagda RY, Vazquez-Mayorga E, Martinez B, Gallahue A. Intranasal Administration of Forskolin and Noopept Reverses Parkinsonian Pathology in PINK1 Knockout Rats. Int J Mol Sci. 2022 Dec 30;24(1):690. doi: 10.3390/ijms24010690. PMID: 36614135; PMCID: PMC9820624.
4. Chen JY, Peng SY, Cheng YH, Lee IT, Yu YH. Effect of Forskolin on Body Weight, Glucose Metabolism and Adipocyte Size of Diet-Induced Obesity in Mice. Animals (Basel). 2021 Mar 1;11(3):645. doi: 10.3390/ani11030645. PMID: 33804418; PMCID: PMC8000574.
In vitro protocol:
1. Tsai HW, Lin VY, Shupnik MA. Forskolin Stimulates Estrogen Receptor (ER) α Transcriptional Activity and Protects ER from Degradation by Distinct Mechanisms. Int J Endocrinol. 2022 May 9;2022:7690166. doi: 10.1155/2022/7690166. PMID: 35586275; PMCID: PMC9110234.
2. Yang P, Jiang PW, Li C, Gao MX, Sun YS, Zhang DY, Du WQ, Zhao J, Shi ST, Li Y, Yang T, Cheng L, Li MH. Cdc25C/cdc2/cyclin B, raf/MEK/ERK and PERK/eIF2α/CHOP pathways are involved in forskolin-induced growth inhibition of MM.1S cells by G2/M arrest and mitochondrion-dependent apoptosis. Cell Cycle. 2021 Nov;20(22):2402-2412. doi: 10.1080/15384101.2021.1983280. Epub 2021 Oct 4. PMID: 34606419; PMCID: PMC8794531.
In vivo protocol:
1. Dagda RK, Dagda RY, Vazquez-Mayorga E, Martinez B, Gallahue A. Intranasal Administration of Forskolin and Noopept Reverses Parkinsonian Pathology in PINK1 Knockout Rats. Int J Mol Sci. 2022 Dec 30;24(1):690. doi: 10.3390/ijms24010690. PMID: 36614135; PMCID: PMC9820624.
2. Chen JY, Peng SY, Cheng YH, Lee IT, Yu YH. Effect of Forskolin on Body Weight, Glucose Metabolism and Adipocyte Size of Diet-Induced Obesity in Mice. Animals (Basel). 2021 Mar 1;11(3):645. doi: 10.3390/ani11030645. PMID: 33804418; PMCID: PMC8000574.
1: St John HC, Hansen SJ, Pike JW. Analysis of SOST expression using large minigenes reveals the MEF2C binding site in the evolutionarily conserved region (ECR5) enhancer mediates forskolin, but not 1,25-dihydroxyvitamin D(3) or TGFβ(1) responsiveness. J Steroid Biochem Mol Biol. 2015 Sep 7. pii: S0960-0760(15)30063-7. doi: 10.1016/j.jsbmb.2015.09.005. [Epub ahead of print] Review. PubMed PMID: 26361013; PubMed Central PMCID: PMC4781661.
2: Wagh VD, Patil PN, Surana SJ, Wagh KV. Forskolin: upcoming antiglaucoma molecule. J Postgrad Med. 2012 Jul-Sep;58(3):199-202. Review. PubMed PMID: 23023353.
3: Alasbahi RH, Melzig MF. Forskolin and derivatives as tools for studying the role of cAMP. Pharmazie. 2012 Jan;67(1):5-13. Review. PubMed PMID: 22393824.
4: Insel PA, Ostrom RS. Forskolin as a tool for examining adenylyl cyclase expression, regulation, and G protein signaling. Cell Mol Neurobiol. 2003 Jun;23(3):305-14. Review. PubMed PMID: 12825829.
5: De Souza NJ. Industrial development of traditional drugs: the forskolin example. A mini-review. J Ethnopharmacol. 1993 Mar;38(2-3):177-80. Review. PubMed PMID: 8510466.
6: Bhat SV. Forskolin and congeners. Fortschr Chem Org Naturst. 1993;62:1-74. Review. PubMed PMID: 8349218.
7: Laurenza A, Sutkowski EM, Seamon KB. Forskolin: a specific stimulator of adenylyl cyclase or a diterpene with multiple sites of action? Trends Pharmacol Sci. 1989 Nov;10(11):442-7. Review. PubMed PMID: 2692256.
8: Schlepper M, Thormann J, Mitrovic V. Cardiovascular effects of forskolin and phosphodiesterase-III inhibitors. Basic Res Cardiol. 1989;84 Suppl 1:197-212. Review. PubMed PMID: 2530974.
9: Georgieva Zh, Uzunov P. [The diterpene forskolin--a valuable agent for demonstrating the role of the cyclic 3',5'-adenosine monophosphate system in physiological processes]. Eksp Med Morfol. 1988;27(1):56-61. Review. Bulgarian. PubMed PMID: 2836155.
10: Seamon KB, Daly JW. Forskolin: its biological and chemical properties. Adv Cyclic Nucleotide Protein Phosphorylation Res. 1986;20:1-150. Review. PubMed PMID: 3028083.
11: Ammon HP, Müller AB. Forskolin: from an ayurvedic remedy to a modern agent. Planta Med. 1985 Dec;(6):473-7. Review. PubMed PMID: 3006108.
12: Mokhtari A, Do Khac L, Tanfin Z, Harbon S. Forskolin modulates cyclic AMP generation in the rat myometrium. Interactions with isoproterenol and prostaglandins E2 and I2. J Cyclic Nucleotide Protein Phosphor Res. 1985;10(3):213-27. Review. PubMed PMID: 2991348.
13: Daly JW. Forskolin, adenylate cyclase, and cell physiology: an overview. Adv Cyclic Nucleotide Protein Phosphorylation Res. 1984;17:81-9. Review. PubMed PMID: 6328947.
14: Hedin L, Rosberg S. Forskolin effects on the cAMP system and steroidogenesis in the immature rat ovary. Mol Cell Endocrinol. 1983 Nov;33(1):69-80. Review. PubMed PMID: 6315510.
15: Sano M. [Forskolin and adenylate cyclase]. Tanpakushitsu Kakusan Koso. 1983 Jun;28(7):943-50. Review. Japanese. PubMed PMID: 6351176.
16: de Souza NJ, Dohadwalla AN, Reden J. Forskolin: a labdane diterpenoid with antihypertensive, positive inotropic, platelet aggregation inhibitory, and adenylate cyclase activating properties. Med Res Rev. 1983 Apr-Jun;3(2):201-19. Review. PubMed PMID: 6345959.
17: Seamon KB, Daly JW. Forskolin: a unique diterpene activator of cyclic AMP-generating systems. J Cyclic Nucleotide Res. 1981;7(4):201-24. Review. PubMed PMID: 6278005.
