Nisoldipine
(Synonyms: 尼索地平; BAY-k 5552) 目录号 : GC16889
A calcium channel inhibitor
Cas No.:63675-72-9
Sample solution is provided at 25 µL, 10mM.
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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
| Kinase experiment [1]: | |
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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]: | |
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Cell lines |
Guinea-pig ventricular myocytes |
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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]: | |
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Animal models |
A dog model of coronary ischemia-reperfusion |
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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. |
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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. |
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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. | |
| Cas No. | 63675-72-9 | SDF | |
| 别名 | 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 | ||
| Canonical 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 |
| 溶解度 | ≥ 11.55mg/mL in DMSO | 储存条件 | 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℃，然后在超声波浴中震荡一段时间。 |
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| 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。 | ||
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 2.5746 mL | 12.873 mL | 25.746 mL |
| 5 mM | 0.5149 mL | 2.5746 mL | 5.1492 mL |
| 10 mM | 0.2575 mL | 1.2873 mL | 2.5746 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet