344270

Forskolin, Coleus forskohlii

• 別名: Forskolin, Coleus forskohlii, 7β-Acetoxy-8,13-epoxy-1α,6β,9α-trihydroxy-labd-14-en-11-one, Colforsin
• 実験式（ヒル表記法）: C₂₂H₃₄O₇
• CAS番号: 66575-29-9
• 分子量: 410.50
• MDL番号: MFCD00082317
• UNSPSCコード: 12352200

特性

• アッセイ: ≥99% (HPLC)
• 品質水準: 100
• 形状: crystalline solid
• メーカー／製品名: Calbiochem^®
• 保管条件: OK to freeze
• 色: white to off-white
• 溶解性: DMSO: 5 mg/mL
• 輸送温度: ambient
• 保管温度: 10-30°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

詳細

詳細

A cardioactive diterpene isolated from the Indian plant Coleus forskolii. At low doses, acts as a positive inotropic agent in dogs, cats, spontaneously hypertensive and normal rats, and isolated guinea pig heart. At higher doses, acts as a hypotensive and vasodilatory agent due to its action as a smooth muscle relaxant. No major side effects are observed at effective doses. Rapid and reversible activator of adenylate cyclase (EC₅₀ = 4 µM) in membranes and intact cells. Does not affect the activity of guanylate cyclase or cyclic nucleotide phophodiesterases. The exact mechanism of forskolin′s positive inotropic effect is unknown but may be related to a cAMP-dependent increase in Na⁺ permeability, which results in indirect augmentation of Ca²⁺ release. Inhibits MAP kinase in rat renal mesangial cells (IC₅₀ = 25 µM). Also acts as a Hh pathway antagonist. Shown to inhibit apoptosis in cerebellar granule cells and to induce apoptosis in resting human B-lymphocytes.

The major cell-permeable diterpene isolated from the Indian plant Coleus forskohlii. At low doses, it acts as a positive inotropic agent. At higher doses, it serves as a hypotensive and vasodilatory agent due to its actions as a smooth muscle relaxant. No major side effects are observed at effective doses. Forskolins pharmacological activities are due to its activation of adenylate cyclase (EC₅₀ = 4 µM), resulting in increased cAMP levels. The exact mechanism of forskolins positive inotropic effect is unknown but may be related to a cAMP-dependent increase in Na⁺ permeability that results in indirect augmentation of Ca²⁺ release. Inhibits MAP kinase in rat renal mesangial cells (IC₅₀ = 25 µM). Also acts as a Hh pathway antagonist. Shown to inhibit apoptosis in cerebellar granule cells and to induce apoptosis in resting human B lymphocytes.

生物化学的／生理学的作用

Cell permeable: yes

Product does not compete with ATP.

Reversible: no

Target IC₅₀: 25 µM inhibiting MAP kinase in rat renal mesangial cells; EC50 = 4 µM for activation of adenylate cyclase

注意

Ethanol is reported to inhibit forskolin-mediated activation of adenylate cyclase. DMSO is the recommended solvent; at ≤5% DMSO final concentration, little inhibition of the adenylate cyclase activation will occur.

警告

Toxicity: Harmful (C)

再構成

Following reconstitution, store in the refrigerator (4°C). DMSO stock solutions are stable for up to 4 months at 4°C.

その他情報

D′Orazio, J.A., et al. 2006. Nature443, 340.
Noveen, A., et al. 1996. Biochem. Biophys. Res. Commun.219, 180.
Galli, C., et al. 1995. J. Neurosci.15, 1172.
Li, X., et al. 1995. Am. J. Physiol.269, C986.
Lomo, J., et al. 1995. J. Immunol.154, 1634.
Uneyama, H., et al. 1993. J. Biol. Chem.268, 168.
Laurenza, A., et al. 1989. Trends Pharmacol. Sci.10, 442.
Adashi, E.Y., and Resnick, C.E. 1986. J. Cell. Biochem.31, 217.
Seamon, K.B., and Daly, J.W. 1986. Adv. Cyclic Nucleotide Protein Phosphorylation Res.20, 1.
Huang, R., et al. 1982. Cyclic Nucleotide Res.8, 385.
Metzger, H., and Lindner, E. 1981. IRCS Med. Sci. Biochem. Cardiovasc. System Pharmacol.9, 99.

法的情報

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

安全性情報

• ピクトグラム: GHS07
• シグナルワード: Warning
• 危険有害性情報: H312
• 注意書き: P280 - P302 + P352 + P312 - P362 + P364 - P501
• 危険有害性の分類: Acute Tox. 4 Dermal
• 保管分類コード: 11 - Combustible Solids
• WGK: WGK 3