Nicorandil-SG-75-DataSheet-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemENicorandilCat. No.: HY-B0341CAS No.: 65141-46-0Synonyms: SG-75分式: CHNO分量: 211.17作靶點: Potassium Channel作通路: Membrane Transporter/Ion Channel儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 DMSO : 33

2、 mg/mL (156.27 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 4.7355 mL 23.6776 mL 47.3552 mL5 mM 0.9471 mL 4.7355 mL 9.4710 mL10 mM 0.4736 mL 2.3678 mL 4.7355 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。BIOLOGICAL ACTIVITY物活性 Nicorandil (SG-75) 鉀離通道活

3、化劑。IC50 & Target Potassium Channel 1.體外研究Nicorandil (SG-75) is a vasodilatory drug used to treat angina. Nicorandil (SG-75) stimulates guanylate1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEcyclase to increase formation of cyclic GMP (cGMP). cGMP activates protein kinase G (PKG) whichphosphorylat

4、es and inhibits GTPase RhoA and decreases Rho-kinase activity. Reduced Rho-kinase activitypermits an increase in myosin phosphatase activity, decreasing the calcium sensitivity of the smooth muscle.PKG also activates the sarcolemma calcium pump to remove activating calcium. PKG acts on K+ channels t

5、opromote K+ efflux and the ensuing hyperpolarization inhibits voltage-gated calcium channels. Overall, thisleads to relaxation of the smooth muscle and coronary vasodilation 1 2.REFERENCES1. Nakae, I., et al., Effects of intravenous nicorandil on coronary circulation in humans: plasma concentration

6、and action mechanism. JCardiovasc Pharmacol, 2000. 35(6): p. 919-25.2. Sauzeau, V., et al., Cyclic GMP-dependent protein kinase signaling pathway inhibits RhoA-induced Ca2+ sensitization of contraction invascular smooth muscle. J Biol Chem, 2000. 275(28): p. 21722-9.McePdfHeightCaution: Product has not been fully validated for medical applications.For research use only.Tel: 400-