Nicorandil

製品コードS1971 バッチS197101

化学情報

	Synonyms	SG-75	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₈H₉N₃O₄
	分子量	211.17	CAS No.	65141-46-0
Solubility (25°C)*	体外	DMSO	42 mg/mL (198.89 mM)
		Ethanol	42 mg/mL (198.89 mM)
		Water	17 mg/mL (80.5 mM)
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	Nicorandil (SG-75) is a potassium channel activator, and stimulates guanylate cyclase to increase formation of cyclic GMP (cGMP).
in vitro	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. ^[1] 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). ^[2] 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. ^[3] 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. ^[4]
in vivo	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. ^[5]

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: , , J Cardiovasc Pharmacol Ther, 2016, 21(6):549-562.

: Data from [Data independently produced by , , Sci Rep, 2017, 7(1):3156]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

A Long-Term Study Evaluating the Effects of Nicorandil Treatment on Duchenne Muscular Dystrophy-Associated Cardiomyopathy in mdx Mice [ J Cardiovasc Pharmacol Ther, 2022, 27:10742484221088655]	PubMed: 35353647
Cardioprotective effect of nicorandil on isoproterenol induced cardiomyopathy in the Mdx mouse model [ BMC Cardiovasc Disord, 2021, 21(1):302]	PubMed: 34130633
Modeling Congenital Hyperinsulinism with ABCC8-Deficient Human Embryonic Stem Cells Generated by CRISPR/Cas9. [Guo D, et al. Sci Rep, 2017, 7(1):3156]	PubMed: 28600547
Nicorandil, a Nitric Oxide Donor and ATP-Sensitive Potassium Channel Opener, Protects Against Dystrophin-Deficient Cardiomyopathy [Afzal MZ, et al. J Cardiovasc Pharmacol Ther, 2016, 10.1177/1074248416636477]	PubMed: 26940570

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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