CAS NO: | 2016-88-8 |
包装 | 价格(元) |
10 mM * 1 mL in DMSO | 电议 |
100mg | 电议 |
500mg | 电议 |
1 g | 电议 |
5 g | 电议 |
生物活性 | Amiloride hydrochloride (MK-870 hydrochloride) is an inhibitor of both epithelialsodium channel(ENaC[1]) and urokinase-type plasminogen activator receptor (uTPA[2]). Amiloride hydrochloride is a blocker ofpolycystin-2(PC2;TRPP2[3]) channel. | ||||||||||||||||
IC50& Target | ENaC[1]; uTPA[2]; polycystin-2(TRPP2)[3] | ||||||||||||||||
体外研究 (In Vitro) | Amiloride blocks δβγ channels with an IC50of 2.6 μM. The Kiof amiloride for δβγ ENaC is 26-fold that of αβγ channels (0.1 μM for αβγ ENaC). Amiloride blockade of δβγ ENaC is much more voltage dependent compared with the αβγ channel. The Kiof amiloride for δαβγ channels is 920 and 13.7 μM at –120 and+80 mV, respectively, which significantly differs from that of both αβγ and δβγ channels[1]. Amiloride is a relatively selective inhibitor of the epithelial sodium channel (ENaC) with an IC50(the concentration required to reach 50% inhibition of an ion channel) in the concentration range of 0.1 to 0.5 μM. Amiloride is a relatively poor inhibitor of the the Na+/H+exchanger (NHE) with an IC50as low as 3 μM in the presence of a low external [Na+] but as high as 1 mM in the presence of a high [Na+]. Amiloride is an even weaker inhibitor of the Na+/Ca2+exchanger (NCX), with an IC50of 1 mM. Amiloride (1 μM) and submicromolar doses of Benzamil (30 nM), doses known to inhibit the ENaC, inhibit the myogenic vasoconstriction response to increasing perfusion pressure by blocking the activity of ENaC proteins. Amiloride completely inhibits Na+influx in doses known to be relatively specific for ENaC (1.5 μM) in vascular smooth muscle cells (VSMC)[2]. | ||||||||||||||||
体内研究 (In Vivo) | Amiloride (1 mg/kg/day) subcutaneously is found to reverse the initial increases in collagen deposition and prevent any further increases in the DOCA-salt hypertensive rat. Amiloride delays the onset of proteinuria and improved brain and kidney histologic scores in the saline-drinking, stroke-prone spontaneously hypertensive rats (SHRSP) compared with controls. Amiloride antagonizes or prevents actions of aldosterone in these cells and in cardiovascular and renal tissues in animals with salt-dependent forms of hypertension[2]. | ||||||||||||||||
Clinical Trial | |||||||||||||||||
分子量 | 266.09 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C6H9Cl2N7O | ||||||||||||||||
CAS 号 | 2016-88-8 | ||||||||||||||||
中文名称 | 盐酸阿米洛利 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) | ||||||||||||||||
溶解性数据 | In Vitro: DMSO : ≥ 100 mg/mL(375.81 mM) H2O : 7.14 mg/mL(26.83 mM;Need ultrasonic) *"≥" means soluble, but saturation unknown. 配制储备液
* 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。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用;
以下溶剂前显示的百
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