生物活性
Amiloride hydrochloride dihydrate is a potent epithelial sodium channel blocker. Amilorida is the hydrochloride dehydrate of amiloride. Amiloride hydrochloride dihydrate works by directly blocking the epithelial sodium channel thereby inhibiting sodium reabsorption in the late distal convoluted tubules, connecting tubules, and collecting ducts in the kidneys (this mechanism is the same for triamterene). This promotes the loss of sodium and water from the body, but without depleting potassium. Amiloride hydrochloride dihydrate also carries the risk of developing an acidosis. A fraction of the effects of amiloride is inhibition of cyclic GMP-gated cation channels in the inner medullary collecting duct. Amiloride hydrochloride dihydrate has a second action on the heart, blocking Na+/H+ exchangers Sodium-hydrogen antiporter 1 or NHE-1. This minimizes reperfusion injury in ischemic attacks. Acid-Sensing ion channels are also sensitive to inhibition by Amiloride hydrochloride dihydrate.
化学数据
| 分子量 | 302.12 |
| 分子式 | C6H8ClN7O.HCl.2H2O |
| CAS号 | 17440-83-4 |
| 纯度 | >99% |
| 溶解性（25°C） | DMSO 50 mg/mL |
| 储存和运输条件 | 固体粉末： -20°C 冷藏长期储存
常温运输及临时存放 |
不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）
| 小鼠 | 大鼠 | 兔 | 豚鼠 | 仓鼠 | 狗 |
| 重量 (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| 体表面积 (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km系数 | 3 | 6 | 12 | 8 | 5 | 20 |
| 动物 A (mg/kg) = 动物 B (mg/kg) × | 动物 B的Km系数 |
| 动物 A的Km系数 |
例如，依据体表面积折算法，将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量，需要将20 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到化合物用于大鼠的等效剂量为10 mg/kg。
储备液配制
以下数据基于产品分子量，对于特殊产品，请参照COA中的储备液配制条件和说明进行操作。
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 3.3099 mL | 16.5497 mL | 33.0994 mL |
| 5 mM | 0.662 mL | 3.3099 mL | 6.6199 mL |
| 10 mM | 0.331 mL | 1.655 mL | 3.3099 mL |
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