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Amiloride hydrochloride dihydrate

Cat. No. M3366
Amiloride hydrochloride dihydrate Structure
Synonym:

MK-870 hydrochloride dihydrate

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
100mg USD 60  USD60 In stock
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Quality Control & Documentation
Biological Activity

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.

Product Citations
Chemical Information
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
Conversion of different model animals based on BSA (PMID: 27057123)
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.

References

[1] D Leppla, et al. Effect of amiloride with or without hydrochlorothiazide on urinary calcium and saturation of calcium salts

[2] J E Baer, et al. The potassium-sparing and natriuretic activity of N-amidino-3,5-diamino-6-chloropyrazinecarboxamide hydrochloride dihydrate (amiloride hydrochloride)

[3] W J Goldman, et al. Effects of the chronic administration of amiloride hydrochloride (N-amidino-3,5-diamino-6-chloropyrazinecarboxamide hydrochloride dihydrate) on electrolyte balance in the dog

[4] A K Ho, et al. Inhibitory effects of amilorides on pinealocyte adenosine 3',5'-monophosphate and guanosine 3',5'-monophosphate accumulation: possible involvement of postreceptor mechanisms

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Keywords: Amiloride hydrochloride dihydrate, MK-870 hydrochloride dihydrate supplier, Sodium Channel, inhibitors, activators


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