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product name
Forskolin, Coleus forskohlii,
アッセイ
≥99% (HPLC)
品質水準
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
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.
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
シグナルワード
Warning
危険有害性情報
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
適用法令
試験研究用途を考慮した関連法令を主に挙げております。化学物質以外については、一部の情報のみ提供しています。 製品を安全かつ合法的に使用することは、使用者の義務です。最新情報により修正される場合があります。WEBの反映には時間を要することがあるため、適宜SDSをご参照ください。
Jan Code
344270-250MG:
344270-50MG:
344270-MG:
344270-300MG:
344270-10MG:
344270-25MG:
344270-1.1ML:
試験成績書（COA）
製品のロット番号・バッチ番号を入力して、試験成績書（COA） を検索できます。ロット番号・バッチ番号は、製品ラベルに「Lot」または「Batch」に続いて記載されています。
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