Amiloride Hydrochloride Dihydrate (MK-870 Hydrochloride Dihydrate) is an inhibitor of epithelial sodium channel (ENaC) and urokinase-type plasminogen activator receptor (uTPA). Amiloride hydrochloride dihydrate is polycystin-2 (PC2; TRPP2) channel blocker. 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.
J Med Virol. 2023 Jan;95(1).
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Amiloride hydrochloride dihydrate purchased from AbMole
Molecular Weight | 302.12 |
Formula | C6H8ClN7O.HCl.2H2O |
CAS Number | 17440-83-4 |
Solubility (25°C) | DMSO ≥ 60 mg/mL Water 2 mg/mL |
Storage | -20°C, dry, sealed |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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