Amiloride Hydrochloride

    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 319532

CAS#: 17440-83-4

Description: Amiloride is a potassium-sparing diuretic, first approved for use in 1967 (then known as MK 870), used in the management of hypertension and congestive heart failure. Amiloride works by directly blocking the epithelial sodium channel (ENaC) 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.

Chemical Structure

Amiloride Hydrochloride
CAS# 17440-83-4

Theoretical Analysis

MedKoo Cat#: 319532
Name: Amiloride Hydrochloride
CAS#: 17440-83-4
Chemical Formula: C6H13Cl2N7O3
Exact Mass: 301.0457
Molecular Weight: 302.116
Elemental Analysis: C, 23.85; H, 4.34; Cl, 23.47; N, 32.45; O, 15.89

Price and Availability

Size Price Availability Quantity
1.0g USD 80.0 2 Weeks
2.0g USD 150.0 2 Weeks
5.0g USD 350.0 2 Weeks
10.0g USD 650.0 2 Weeks
20.0g USD 950.0 2 Weeks
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Synonym: MK870; MK-870; MK 870; Amiloride Hydrochloride; Midamor; Midoride; Modamide.

IUPAC/Chemical Name: Pyrazinecarboxamide, 3,5-diamino-N-(aminoiminomethyl)-6-chloro-, monohydrochloride dihydrate


InChi Code: 1S/C6H8ClN7O.ClH.2H2O/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;2*1H2

SMILES Code: c1(c(nc(c(n1)Cl)N)N)C(=O)NC(=N)N.O.O.Cl

Appearance: Light yellow to yellow solid powder.

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

Preparing Stock Solutions

The following data is based on the product molecular weight 302.116 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL

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1: Judd EK, Calhoun DA, Warnock DG. Pathophysiology and treatment of resistant hypertension: the role of aldosterone and amiloride-sensitive sodium channels. Semin Nephrol. 2014;34(5):532-9. doi: 10.1016/j.semnephrol.2014.08.007. Review. PubMed PMID: 25416662; PubMed Central PMCID: PMC4450367.

2: Warnock DG, Kusche-Vihrog K, Tarjus A, Sheng S, Oberleithner H, Kleyman TR, Jaisser F. Blood pressure and amiloride-sensitive sodium channels in vascular and renal cells. Nat Rev Nephrol. 2014 Mar;10(3):146-57. doi: 10.1038/nrneph.2013.275. Epub 2014 Jan 14. Review. PubMed PMID: 24419567; PubMed Central PMCID: PMC4137491.

3: Ji HL, Zhao RZ, Chen ZX, Shetty S, Idell S, Matalon S. δ ENaC: a novel divergent amiloride-inhibitable sodium channel. Am J Physiol Lung Cell Mol Physiol. 2012 Dec 15;303(12):L1013-26. doi: 10.1152/ajplung.00206.2012. Epub 2012 Sep 14. Review. PubMed PMID: 22983350; PubMed Central PMCID: PMC3532584.

4: Matthews H, Ranson M, Kelso MJ. Anti-tumour/metastasis effects of the potassium-sparing diuretic amiloride: an orally active anti-cancer drug waiting for its call-of-duty? Int J Cancer. 2011 Nov 1;129(9):2051-61. doi: 10.1002/ijc.26156. Epub 2011 Aug 1. Review. PubMed PMID: 21544803.

5: O'Brodovich H, Yang P, Gandhi S, Otulakowski G. Amiloride-insensitive Na+ and fluid absorption in the mammalian distal lung. Am J Physiol Lung Cell Mol Physiol. 2008 Mar;294(3):L401-8. Epub 2007 Dec 27. Review. PubMed PMID: 18162600.

6: Teiwes J, Toto RD. Epithelial sodium channel inhibition in cardiovascular disease. A potential role for amiloride. Am J Hypertens. 2007 Jan;20(1):109-17. Review. PubMed PMID: 17198922.

7: Haddad JJ. Amiloride and the regulation of NF-kappaB: an unsung crosstalk and missing link between fluid dynamics and oxidative stress-related inflammation--controversy or pseudo-controversy? Biochem Biophys Res Commun. 2005 Feb 11;327(2):373-81. Review. PubMed PMID: 15629126.

8: Swift PA, MacGregor GA. The epithelial sodium channel in hypertension: genetic heterogeneity and implications for treatment with amiloride. Am J Pharmacogenomics. 2004;4(3):161-8. Review. PubMed PMID: 15174897.

9: Hirsh AJ. Altering airway surface liquid volume: inhalation therapy with amiloride and hyperosmotic agents. Adv Drug Deliv Rev. 2002 Dec 5;54(11):1445-62. Review. PubMed PMID: 12458154.

10: Guggino WB, Guggino SE. Amiloride-sensitive sodium channels contribute to the woes of the flu. Proc Natl Acad Sci U S A. 2000 Aug 29;97(18):9827-9. Review. PubMed PMID: 10963654; PubMed Central PMCID: PMC34034.

11: Alvarez de la Rosa D, Canessa CM, Fyfe GK, Zhang P. Structure and regulation of amiloride-sensitive sodium channels. Annu Rev Physiol. 2000;62:573-94. Review. PubMed PMID: 10845103.

12: Wazny LD, Brophy DF. Amiloride for the prevention of amphotericin B-induced hypokalemia and hypomagnesemia. Ann Pharmacother. 2000 Jan;34(1):94-7. Review. PubMed PMID: 10669191.

13: Kleyman TR, Sheng S, Kosari F, Kieber-Emmons T. Mechanism of action of amiloride: a molecular prospective. Semin Nephrol. 1999 Nov;19(6):524-32. Review. PubMed PMID: 10598540.

14: Karmazyn M. The role of the myocardial sodium-hydrogen exchanger in mediating ischemic and reperfusion injury. From amiloride to cariporide. Ann N Y Acad Sci. 1999 Jun 30;874:326-34. Review. PubMed PMID: 10415544.

15: Harris C, Fliegel L. Amiloride and the Na(+)/H(+) exchanger protein: mechanism and significance of inhibition of the Na(+)/H(+) exchanger (review). Int J Mol Med. 1999 Mar;3(3):315-21. Review. PubMed PMID: 10028059.

16: Halpern BP. Amiloride and vertebrate gustatory responses to NaCl. Neurosci Biobehav Rev. 1998;23(1):5-47. Review. PubMed PMID: 9861611.

17: Horisberger JD. Amiloride-sensitive Na channels. Curr Opin Cell Biol. 1998 Aug;10(4):443-9. Review. PubMed PMID: 9719863.

18: Hummler E. Reversal of convention: from man to experimental animal in elucidating the function of the renal amiloride-sensitive sodium channel. Exp Nephrol. 1998 Jul-Aug;6(4):265-71. Review. PubMed PMID: 9690087.

19: Voilley N, Galibert A, Bassilana F, Renard S, Lingueglia E, Coscoy S, Champigny G, Hofman P, Lazdunski M, Barbry P. The amiloride-sensitive Na+ channel: from primary structure to function. Comp Biochem Physiol A Physiol. 1997 Oct;118(2):193-200. Review. PubMed PMID: 9366043.

20: Blazer-Yost BL, Helman SI. The amiloride-sensitive epithelial Na+ channel: binding sites and channel densities. Am J Physiol. 1997 Mar;272(3 Pt 1):C761-9. Review. PubMed PMID: 9124509.