A potassium-sparing diuretic
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Analytical Standard(s)
26295Amiloride (hydrochloride)
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Amiloride (hydrochloride) (hydrate)

Item No. 14409

Technical Information
Formal Name
3,5-diamino-N-(aminoiminomethyl)-6-chloro-2-pyrazinecarboxamide, monohydrochloride hydrate
Synonyms
  • MK-870
Molecular Formula
C6H8ClN7O • HCl [XH2O]
Formula Weight
Purity
≥98%
Formulation
A crystalline solid
DMF: 30 mg/mlDMSO: 30 mg/mlDMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml
λmax
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
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    Amiloride is a potassium-sparing diuretic.1,2 It is an inhibitor of the epithelial sodium channel (ENaC; K0.5 = 2.6 µM for recombinant δENaC expressed in X. laevis oocytes).3 It inhibits sodium transport from bovine kidney cortex membrane vesicles with an IC50 value of 0.4 µM.4 Amiloride inhibits the urokinase-type plasminogen activator (u-PA; Ki = 7 µM) and cardiac Na+/H+-ATPase (IC50 = 83.8 µM).5,6 It also inhibits calcium currents mediated by transient receptor potential polycystin 3 (TRPP3; IC50 = 143 µM).7 Amiloride (30 mg/kg) reduces mean arterial pressure in spontaneously hypertensive, but not normotensive, rats.8 Formulations containing amiloride have been used alone, and in combination with thiazide diuretics, in the treatment of hypertension.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Lingueglia, E., Voilley, N., Lazdunski, M., et alPhysiological society symposium: Ion channels in health and disease. Molecular biology of the amiloride-sensitive epithelial Na+ channel. Exp. Physiol. 81, 483-492 (1996).

    2. Qadri, Y.J., Rooj, A.K., and Fuller, C.M. ENaCs and ASICs as therapeutic targets. Am. J. Physiol. Cell Physiol. 302(7), C943-C965 (2012).

    3. Waldmann, R., Champigny, G., Bassilana, F., et alMolecular cloning and functional expression of a novel amiloride-sensitive Na+ channel. The Journal of Biological Chemisty 270(46), 27411-27414 (1995).

    4. Kleyman, T.R., Yulo, T., Ashbaugh, C., et alPhotoaffinity labeling of the epithelial sodium channel. The Journal of Biological Chemisty 261(6), 2839-2843 (1986).

    5. Vassalli, J.D., and Belin, D. Amiloride selectively inhibits the urokinase-type plasminogen activator. FEBS Lett. 214(1), 187-191 (1987).

    6. Kleyman, T.R., and Cragoe, E.J., Jr. Amiloride and its analogs as tools in the study of ion transport. J. Membr. Biol. 105(1), 1-21 (1988).

    7. Dai, X.Q., Ramji, A., Liu, Y., et alInhibition of TRPP3 channel by amiloride and analogs. Mol. Pharmacol. 72(6), 1576-1585 (2007).

    8. Barrett, R.J., and Kau, S.T. Myocardial and vascular actions of amiloride in spontaneously hypertensive rats. J. Pharmacol. Exp. Ther. 239(2), 365-374 (1986).