| 包装 | 价格(元) |
| 10mM (in 1mL DMSO) | 电议 |
| 200mg | 电议 |
| 500mg | 电议 |
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 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 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 ℃ 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 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. |
| 产品描述 | 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: |
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