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Nisoldipine (BAY-k 5552) 是一种高效特异的L 型Cav1.2通道阻断剂,IC50=10 nM。
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Nisoldipine (BAY-k 5552) 是一种高效特异的L 型Cav1.2通道阻断剂,IC50=10 nM。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
25 mg | ¥ 169 | 现货 | |
50 mg | ¥ 233 | 现货 | |
100 mg | ¥ 328 | 现货 | |
500 mg | ¥ 529 | 现货 | |
1 g | ¥ 793 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 150 | 现货 |
产品描述 | Nisoldipine (BAY-k 5552) is a dihydropyridine calcium channel antagonist that acts as a potent arterial vasodilator and antihypertensive agent. |
靶点活性 | Cav 1.2, L-type:10 nM |
体外活性 | 对于Timothy综合征病人,Nisoldipine(IC50=267 nM)通过抑制钙离子从L型钙通道流入,降低动脉平滑肌收缩性及随后的血管收缩 , 导致血管舒张,且降低血压. |
体内活性 | 在豚鼠心室肌细胞中,Nisoldipine延迟整流K+通道,快速激活延迟整流K+通道抑制IKr(IC50=23 μM), 及缓慢激活延迟整流K+通道抑制IKs(IC50=40 μM)。 |
激酶实验 | Binding experiments of electrophysiology: 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. |
细胞实验 | 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.(Only for Reference) |
别名 | 尼索地平, BAY-k 5552 |
分子量 | 388.41 |
分子式 | C20H24N2O6 |
CAS No. | 63675-72-9 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
溶解度信息 | Ethanol: 56 mg/mL (144.2 mM) H2O: < 1 mg/mL (insoluble or slightly soluble) DMSO: 50 mg/mL (128.73 mM) | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
DMSO/Ethanol
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