GlpBio

Nisoldipine

目录号: GC16889纯度: >99.00%同义词: 尼索地平; BAY-k 5552
A calcium channel inhibitor
Nisoldipine
Cas No.: 63675-72-9
规格价格库存数量操作
100mg¥280.00现货
1
500mg¥448.00现货
1
1g¥686.00现货
1
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产品描述 Description

Nisoldipine(BAY-k 5552; Sular) is a calcium channel blocker belonging to the dihydropyridines class, specific for L-type Cav1.2 with IC50 of 10 nM. IC50 value: 10 nMTarget: L-type Cav1.2Nisoldipine 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. Nisoldipine is about 30 times less selective for delayed-rectifier K+ channels than for L-type Ca2+ channels, which inhibits IKr (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. Nisoldipine also displays antioxidant potency with IC50 of 28.2 μM both before and after the addition of active oxygen.

References:
[1]. Hamilton SF, Houle LM, Thadani U. Rapid-release and coat-core formulations of nisoldipine in treatment of hypertension, angina, and heart failure. Heart Dis. 1999 Nov-Dec;1(5):279-88.
[2]. Fodor JG. Nisoldipine CC: efficacy and tolerability in hypertension and ischemic heart disease. Cardiovasc Drugs Ther. 1997 Jan;10 Suppl 3:873-9.
[3]. D.J. Duncker, J.M. Hartog, P.G. Hugenholtz, et al. The effects of nisoldipine (Bay K 5552) on cardiovascular performance and regional blood flow in pentobarbital - anaesthetized pigs with or without β-adrenoceptor blockade. British Journal of Pharmacology. 1986,88(1): 9-18
[4]. Jan W. De Jong, Tom Huizer, Jan G.P. Tijssen. Energy conservation by nisoldipine in ischaemic heart. British Journal of Pharmacology. 1984, 83(4): 943-949

实验参考方法 Experimental Reference Method

Kinase experiment [1]:

Binding experiments of electrophysiology

CHO cells expressing the subunit of the voltage-dependent L-type Ca2+ channel were 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 was 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 IC50 values were calculated.
Cell experiment [2]:

Cell lines

Guinea-pig ventricular myocytes

Preparation method

The solubility of this compound in DMSO is > 11.6 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months.

Reacting condition

10 ~ 100 μM; 8 ~ 10 mins

Applications

In guinea-pig ventricular myocytes, Nisoldipine inhibited rapidly activating delayed-rectifier K+ current (I(Kr) ) with an IC50 value of 23 μM, as well as slowly activating delayed-rectifier K+ current (I(Ks) ) with an IC50 value of 40 μM. It was estimated that Nisoldipine is approximately 30 times more selective for L-type Ca2+ channels than for delayed-rectifier K+ channels.
Animal experiment [3]:

Animal models

A dog model of coronary ischemia-reperfusion

Dosage form

6.6 μg/kg/min; i.v.

Applications

Compared with the control group, the Nisoldipine treatment group showed similar hemodynamic measurements. However, mass of necrosis and mass at risk was obviously lower in the Nisoldipine group. In a dog model of coronary ischemia-reperfusion, Nisoldipine reduced the infarct size.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Morel N, Buryi V, Feron O, Gomez JP, Christen MO, Godfraind T. The action of calcium channel blockers on recombinant L-type calcium channel alpha1-subunits. Br J Pharmacol. 1998 Nov;125(5):1005-12.

[2]. Missan S1, Zhabyeyev P, Dyachok O, Jones SE, McDonald TF. Block of cardiac delayed-rectifier and inward-rectifier K+ currents by nisoldipine. Br J Pharmacol. 2003 Nov;140(5):863-70.

[3]. Hammerman H, Moscovitz M, Hir J. Beneficial effect of nisoldipine in repeated coronary reperfusion. Coron Artery Dis. 1997 Feb;8(2):97-100.

产品文档 Product Documents

Purity:>99.00%

化学性质Chemical Properties

CAS 号
63675-72-9
同义词
尼索地平; BAY-k 5552
化学名
3-O-methyl 5-O-(2-methylpropyl) 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate
SMILES
CC1=C(C(C(=C(N1)C)C(=O)OCC(C)C)C2=CC=CC=C2[N+](=O)[O-])C(=O)OC
分子式
C20H24N2O6
分子量
388.41 g/mol
溶解性
≥ 11.55mg/mL in DMSO
保存条件
4°C, protect from light
General tips
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
为了提高溶解度，请将管子加热至 37°C，然后在超声波浴中震荡一段时间。
Shipping Condition
评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备 RT，或根据请求配备蓝冰。

计算工具摩尔浓度 / 稀释 / 分子量 / 单位换算 / 体内配方 / 溶解度

g/mol