Amiloride (hydrochloride) (hydrate)

Amiloride is a potassium-sparing diuretic. It is an inhibitor of the epithelial sodium channel (ENaC, K0.5 = 2.6 µM for recombinant deltaENaC expressed in X. laevis oocytes). It inhibits sodium transport from bovine kidney cortex membrane vesicles with an IC50 value of 0.4 µM. Amiloride inhibits the urokinase-type plasminogen activator (u-PA, Ki = 7 µM) and cardiac Na+/H+-ATPase (IC50 = 83.8 µM). It also inhibits calcium currents mediated by transient receptor potential polycystin 3 (TRPP3, IC50 = 143 µM). Amiloride (30 mg/kg) reduces mean arterial pressure in spontaneously hypertensive, but not normotensive, rats. Formulations containing amiloride have been used alone, and in combination with thiazide diuretics, in the treatment of hypertension.Formal Name: 3,5-diamino-N-(aminoiminomethyl)-6-chloro-2-pyrazinecarboxamide, monohydrochloride hydrate. Synonyms: MK-870. Molecular Formula: C6H8ClN7O . HCl [XH2O]. Formula Weight: 266.1. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, DMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml. lambdamax: 215, 287, 362 nm. SMILES: ClC1=C(N)N=C(N)C(C(NC(N)=N)=O)=N1.Cl.O. InChi Code: InChI=1S/C6H8ClN7O.ClH.H2O/c7-2-4(9)13-3(8)1(12-2)5(15)14-6(10)11,,/h(H4,8,9,13)(H4,10,11,14,15),1H,1H2. InChi Key: WDZJJRLYFQNCQL-UHFFFAOYSA-N.