WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H326769
CAS#: 66575-29-9
Description: Forskolin is a naturally occurring diterpene that is produced by the Indian Coleus plant (C. forskohlii). Forskolin modulates cyclic AMP generation in the rat myometrium. Interactions with isoproterenol and prostaglandins E2 and I2. The unique character of forskolin as a general direct, rapid and reversible activator of adenylyl cyclase not only underlies its wide range of pharmacological effects but also renders it as a valuable tool in the study of the role of cAMP.
Hodoodo Cat#: H326769
Name: Forskolin
CAS#: 66575-29-9
Chemical Formula: C22H34O7
Exact Mass: 410.23
Molecular Weight: 410.507
Elemental Analysis: C, 64.37; H, 8.35; O, 27.28
Synonym: Coleonol; HL 362; L 75-1362B; NSC 357088; NSC 375489; Forskolin.
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
Appearance: Solid powder
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
More Info:
Biological target: | Forskolin (Coleonol) 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: | FSK (forskolin) dose‐dependently enhanced EC proliferation (Figure 3A). In contrast, FSK reduced SMC proliferation at high concentrations, 30 or 100 μmol/L (Figure 3B). Reference: J Cell Mol Med. 2020 Sep; 24(17): 9638–9645. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7520276/ |
In vivo activity: | After 3 weeks, the subcutaneous tumor diameter in the forskolin mouse group was larger compared with that in the DMSO group (Fig. 7A). Consistent with the observation in vitro, forskolin treatment resulted in high expression of MMP2, MMP-9 and VE-cad, as well as the activation of the Notch-1 signaling pathway (Fig. 7C). Reference: Int J Oncol. 2020 May; 56(5): 1129–1139. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7115352/ |
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
DMSO | 55.6 | 135.37 | |
DMSO:PBS (pH 7.2) (1:10) | 0.1 | 0.24 | |
DMF | 30.0 | 73.08 | |
Ethanol | 33.7 | 82.09 |
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. Hao H, Ma X, Chen H, Zhu L, Xu Z, Li Q, Xu C, Zhang Y, Peng Z, Wang M. The cyclic adenosine monophosphate elevating medicine, forskolin, reduces neointimal formation and atherogenesis in mice. J Cell Mol Med. 2020 Sep;24(17):9638-9645. doi: 10.1111/jcmm.15476. Epub 2020 Aug 18. PMID: 32810369; PMCID: PMC7520276. 2. Follin-Arbelet V, Misund K, Naderi EH, Ugland H, Sundan A, Blomhoff HK. The natural compound forskolin synergizes with dexamethasone to induce cell death in myeloma cells via BIM. Sci Rep. 2015 Aug 26;5:13001. doi: 10.1038/srep13001. PMID: 26306624; PMCID: PMC4549684. 3. Xue Y, Sun R, Zheng W, Yang L, An R. Forskolin promotes vasculogenic mimicry and invasion via Notch‑1‑activated epithelial‑to‑mesenchymal transition in syncytiolization of trophoblast cells in choriocarcinoma. Int J Oncol. 2020 May;56(5):1129-1139. doi: 10.3892/ijo.2020.4997. Epub 2020 Feb 20. PMID: 32319581; PMCID: PMC7115352. |
In vitro protocol: | 1. Hao H, Ma X, Chen H, Zhu L, Xu Z, Li Q, Xu C, Zhang Y, Peng Z, Wang M. The cyclic adenosine monophosphate elevating medicine, forskolin, reduces neointimal formation and atherogenesis in mice. J Cell Mol Med. 2020 Sep;24(17):9638-9645. doi: 10.1111/jcmm.15476. Epub 2020 Aug 18. PMID: 32810369; PMCID: PMC7520276. 2. Follin-Arbelet V, Misund K, Naderi EH, Ugland H, Sundan A, Blomhoff HK. The natural compound forskolin synergizes with dexamethasone to induce cell death in myeloma cells via BIM. Sci Rep. 2015 Aug 26;5:13001. doi: 10.1038/srep13001. PMID: 26306624; PMCID: PMC4549684. |
In vivo protocol: | 1. Hao H, Ma X, Chen H, Zhu L, Xu Z, Li Q, Xu C, Zhang Y, Peng Z, Wang M. The cyclic adenosine monophosphate elevating medicine, forskolin, reduces neointimal formation and atherogenesis in mice. J Cell Mol Med. 2020 Sep;24(17):9638-9645. doi: 10.1111/jcmm.15476. Epub 2020 Aug 18. PMID: 32810369; PMCID: PMC7520276. 2. Xue Y, Sun R, Zheng W, Yang L, An R. Forskolin promotes vasculogenic mimicry and invasion via Notch‑1‑activated epithelial‑to‑mesenchymal transition in syncytiolization of trophoblast cells in choriocarcinoma. Int J Oncol. 2020 May;56(5):1129-1139. doi: 10.3892/ijo.2020.4997. Epub 2020 Feb 20. PMID: 32319581; PMCID: PMC7115352. |
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.