BMS-191011 (BMS-A) 是一种有效的BKCa通道开启剂 (大电导 Ca2+激活的钾通道)。BMS-191011 在中风的啮齿动物模型中显示出神经保护的活性。
生物活性 | BMS 191011 (BMS-A) is a potentBKCachannelopener (large-conductance Ca2+-activated potassium channel). BMS-191011 shows neuroprotective activities in rodent models of stroke[1]. |
体外研究 (In Vitro) | BMS-191011 (20 or 40 μM) activates BK channels in IGR39 cells, and leads to potentiation in Panc-1 cells[3].
Cell Viability Assay[3] Cell Line: | IGR39 and Panc-1 cells | Concentration: | 20 or 40 μM | Incubation Time: | | Result: | Activated BK channels in less than 50% IGR39 cells and led to less than two-fold potentiation in Panc-1 cells. Promoted the activation of a voltage-independent K+conductance at negative voltages. |
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体内研究 (In Vivo) | BMS-191011 (intravenous injection; 10-100 μg/kg; once) dilates rat retinal arterioles through activation of iberiotoxin-sensitive BK(Ca) channels in vivo[2].
Animal Model: | Male Wistar rats (8- to 10-week-old) treated with Tetrodotoxin (50 μg/kg, intravenously (i.v.))[2] | Dosage: | 10-100 μg/kg | Administration: | Intravenous injection; 10-100 μg/kg; once | Result: | Increased the diameter of retinal arterioles, showed no significant effect on mean arterial pressure and heart rate. |
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | Powder | -20°C | 3 years | | 4°C | 2 years | In solvent | -80°C | 6 months | | -20°C | 1 month |
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溶解性数据 | In Vitro: DMSO : 125 mg/mL(337.19 mM;Need ultrasonic) 配制储备液 1 mM | 2.6975 mL | 13.4876 mL | 26.9753 mL | 5 mM | 0.5395 mL | 2.6975 mL | 5.3951 mL | 10 mM | 0.2698 mL | 1.3488 mL | 2.6975 mL |
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此方案可获得 ≥ 2.08 mg/mL (5.61 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂: 10% DMSO 90%corn oil Solubility: ≥ 2.08 mg/mL (5.61 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (5.61 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。 *以上所有助溶剂都可在本网站选购。
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