344270
Forskolin, Coleus forskohlii
Synonim(y):
Forskolin, Coleus forskohlii, 7β-Acetoxy-8,13-epoxy-1α,6β,9α-trihydroxy-labd-14-en-11-one, Colforsin
Zaloguj sięWyświetlanie cen organizacyjnych i kontraktowych
About This Item
Wzór empiryczny (zapis Hilla):
C22H34O7
Numer CAS:
Masa cząsteczkowa:
410.50
Numer MDL:
Kod UNSPSC:
12352200
Polecane produkty
Próba
≥99% (HPLC)
Poziom jakości
Postać
crystalline solid
producent / nazwa handlowa
Calbiochem®
warunki przechowywania
OK to freeze
kolor
white to off-white
rozpuszczalność
DMSO: 5 mg/mL
Warunki transportu
ambient
temp. przechowywania
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
Klucz InChI
OHCQJHSOBUTRHG-KGGHGJDLSA-N
Opis ogólny
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.
Działania biochem./fizjol.
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
Przestroga
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.
Ostrzeżenie
Toxicity: Harmful (C)
Rekonstytucja
Following reconstitution, store in the refrigerator (4°C). DMSO stock solutions are stable for up to 4 months at 4°C.
Inne uwagi
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.
Informacje prawne
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
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Hasło ostrzegawcze
Warning
Zwroty wskazujące rodzaj zagrożenia
Zwroty wskazujące środki ostrożności
Klasyfikacja zagrożeń
Acute Tox. 4 Dermal
Kod klasy składowania
11 - Combustible Solids
Klasa zagrożenia wodnego (WGK)
WGK 3
Certyfikaty analizy (CoA)
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