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抑制剂/激活剂

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凋亡与自噬

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Amiloride HCl 盐酸阿米洛利

Amiloride HCl是一种选择性的T-type calcium channel阻滞剂，epithelial sodium channel（ENaC）阻滞剂，urokinase plasminogen activator (uPA)抑制剂，Ki=7 μM。

货号：
TK0471
规格：

5mg

10mg

100mg

500mg
价格：
￥0.00

产品参数

CAS No.	2016-88-8
生物活性	Amiloride hydrochloride (MK-870 hydrochloride) is an inhibitor of both epithelial sodium channel (ENaC) and urokinase-type plasminogen activator receptor (uTPA). Amiloride hydrochloride is a blocker of polycystin-2 (PC2; TRPP2) channel.
分子式	C6H9Cl2N7O
分子量	266.09
运输条件	Room temperature in continental US; may vary elsewhere.
溶解性数据	DMSO : ≥ 100 mg/mL (375.81 mM),H2O : 7.14 mg/mL (26.83 mM; Need ultrasonic)
体内研究	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.
体外研究	Amiloride blocks δβγ channels with an IC50 of 2.6 μM. The Ki of 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 Ki of 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. 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 IC50 as 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/Ca exchanger (NCX), with an IC50 of 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).
纯度及产品资料	98%

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