Nisoldipine

製品コードS1748 バッチS174801

化学情報

	Synonyms	BAY K 5552	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₂₀H₂₄N₂O₆
	分子量	388.41	CAS No.	63675-72-9
Solubility (25°C)*	体外	DMSO	78 mg/mL (200.81 mM)
		Ethanol	78 mg/mL warmed with 50ºC water bath (200.81 mM)
		Water	Insoluble
* <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	Nisoldipine (Sular, BAY K 5552) is a calcium channel blocker belonging to the dihydropyridines class, specific for L-type Ca_v1.2 with IC50 of 10 nM.
in vitro	Nisoldipine is a potent blocker of L-type calcium channels. Nisoldipine binds directly to inactive calcium channels stabilizing their inactive conformation Similar to other DHP CCBs. Nisoldipine displays selectivity for arterial smooth muscle cells due to great number of inactive channels and the α1 subunit of the channel. ^[1] Nisoldipine is about 30 times less selective for delayed-rectifier K+ channels than for L-type Ca²⁺ channels, which inhibits I_Kr (rapidly activating delayed-rectifier K⁺ current) with IC50 of 23 μM, and IKs (slowly activating delayed-rectifier K⁺ current)with IC50 of 40 μM in guinea-pig ventricular myocytes. ^[2] Nisoldipine also displays antioxidant potency with IC50 of 28.2 μM both before and after the addition of active oxygen. This is tested by means of rat myocardial membrane lipid peroxidation with a nonenzymatic active oxygen-generating system (DHF/FeC1₃-ADP). ^[3]
in vivo	Nisoldipine decreases arterial smooth muscle contractility and subsequent vasoconstriction by inhibiting the influx of calcium ions through L-type calcium channels. This results in vasodilation and an overall decrease in blood pressure, based on which Nisoldipine is used to treat mild to moderate essential hypertension, chronic stable angina and Prinzmetal's variant angina. ^[4] Nisoldipine shows some ability in patients with Timothy syndrome having Ca_v1.2 missense mutation G406R with IC50 of 267 nM, which is helpful to treat TS. ^[5]
特徴	A member of the dihydropyridine (DHP) class of calcium channel blockers (CCBs), the most widely used class of CCBs.

プロトコル(参考用のみ)

キナーゼアッセイ	Binding experiments of electrophysiology
キナーゼアッセイ	CHO cells expressing the subunit of the voltage-dependent L-type Ca²⁺ channel are cultrured in medium without serum in the presence of different concentrations of Nisoldipine. Then Ca²⁺ channel current elicited from a holding potential of -100 mV or -50 mV is recorded at room temperature with the whole-cell configuration of the patch-clamp method using the List EPC-7 patch-clamp amplifer and pClamp software. The concentration of competitor inhibiting 50% of the specific binding represents IC50.
細胞アッセイ	細胞株	Ventricular myocytes
	濃度	Dissolved in DMSO, final concentration 10-100 μM
	反応時間	8-10 minutes
	実験の流れ	The myocytes are bathed in normal Tyrode's solution, held at -80 mV, and depolarised after 200-ms prepulses (-40mV) to more positive potentials for 500 ms at 0.1 Hz, tail currents are recorded on repolarisations to -40mV. The myocytes are exposed to 10-100 mM Nisoldipine for 8-10 minutes. Then the whole-cell membrane currents are recorded using an EPC-7 amplifier.
動物実験	動物モデル	Male Wistar rats with chronic intragastric ethanol exposure
	投薬量	10 mg/kg
	投与方法	Oral every day

参考

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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：

Calenduloside E protects against myocardial ischemia-reperfusion injury induced calcium overload by enhancing autophagy and inhibiting L-type Ca2+ channels through BAG3 [ Biomed Pharmacother, 2022, 145:112432]	PubMed: 34798472
Deciphering COVID-19 host transcriptomic complexity and variations for therapeutic discovery against new variants [ iScience, 2022, 25(10):105068]	PubMed: 36093376
Trypsin-Mediated Sensitization to Ferroptosis Increases the Severity of Pancreatitis in Mice [ Cell Mol Gastroenterol Hepatol, 2021, S2352-345X(21)00196-X]	PubMed: 34562639
Calcium channel blocker amlodipine besylate therapy is associated with reduced case fatality rate of COVID-19 patients with hypertension [ Cell Discov, 2020, 6(1):96]	PubMed: 33349633
Calenduloside E suppresses calcium overload by promoting the interaction between L-type calcium channels and Bcl2-associated athanogene 3 to alleviate [ Journal of Advanced Research, 2020, 10.1016/j.jare.2020.10.005]	PubMed: None
Reversal of Infected Host Gene Expression Identifies Repurposed Drug Candidates for COVID-19 [ bioRxiv, 2020, 2020/9/20.4.7.30734]	PubMed: 32511305

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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