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抑制剂描述:

产品名称:Nicorandil

产品别名:见爱必信官网

英文别名:Nicorandil

靶点:Potassium Channel

CAS:65141-46-0

纯度:>98%

外观:见爱必信官网

保存方法:Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.

描述:

Nicorandil (Ikorel)is potassium channel activator. It acts by relaxing the smooth muscle of the blood vessels, especially those of the venous system. It does this through two methods. Firstly, by activating potassium channels, and secondly by donating nitric oxide to activate the enzyme guanylate cyclase. Guanylate cyclase causes activation of cGMP leading to both arterial and venous vasodilatation by de-phosphorylation of the myosin light chain.

溶解性:DMSO : >10mg/mL
Water :4.2 mg/mL (20 mM)

体外研究:

Nicorandil (100 mM) increases Flavoprotein oxidation but not membrane current; a 10-fold higher concentration recruits both mitoK(ATP) and surfaceK(ATP) channels. Nicorandil bluntes the rate of cell death in a pelleting model of ischemia; this cardioprotective effect is prevented by the mitoK(ATP) channel blocker 5-hydroxydecanoate but is unaffected by the surfaceK(ATP) channel blocker HMR1098. Nicorandil (100 mM) suppresses TUNEL positivity, cytochrome c translocation, caspase-3 activation and dissipation of mitochondrialinner membrane potential (Delta(Psi)(m)). Nicorandil prevents Delta(Psi)(m) depolarization in a concentration-dependent manner (EC(50) approximately 40 mM, with saturation by 100 mM), as shown by fluorescence-activated cell sorter analysis of cells stained with a fluorescent Delta(Psi)(m)-indicator, tetramethylrhodamine ethyl ester (TMRE). Nicorandil activates a weakly inwardly-rectifying, glibenclamide-sensitive 80 pS K+ channel in both the transfected cells. Nicorandil preferentially activates the K(ATP) channels containing SUR2B in HEK293T cells. Nicorandil (100 mM) significantly suppresses the number of cells with TUNEL-positive nuclei and the increase in caspase-3 activity induced by 20 mM H2O2. Nicorandil prevents the loss of DeltaPsim induced by H2O2 in a concentration-dependent manner.

体内研究:Nicorandil (2.5 mg/kg daily, p.o.) combined with Amlodipine (5.0 mg/kg daily, p.o.) for 3 days significantly prevents these alterations and restored the enzyme activities to near normal in rats.

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