Amiloride HCl

Catalog No.S1811 1 Product Use Citation

Amiloride HCl is a relatively selective inhibitor of the epithelial sodium channel (ENaC), used in the management of hypertension and congestive heart failure.

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Amiloride HCl  Chemical Structure

Amiloride HCl Chemical Structure
Molecular Weight: 266.09

Validation & Quality Control

Quality Control & MSDS

Related Compound Libraries

Amiloride HCl is available in the following compound libraries:

Product Information

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Product Description

Biological Activity

Description Amiloride HCl is a relatively selective inhibitor of the epithelial sodium channel (ENaC), used in the management of hypertension and congestive heart failure.
Targets Sodium channel [1]
In vitro Amiloride is a relatively selective inhibitor of the epithelial sodium channel (ENaC) with an IC50 (the concentration required to reach 50% inhibition of an ion channel) in the concentration range of 0.1 to 0.5 μM. Amiloride is a relatively poor inhibitor of the the Na+/H+ exchanger (NHE) with an IC50 as low as 3 μM in the presence of a low external [Na+] but as high as 1 mM in the presence of a high [Na+]. Amiloride is an even weaker inhibitor of the Na+/Ca2+ exchanger (NCX), with an IC50 of 1 mM. Amiloride (1 μM) and submicromolar doses of Benzamil (30 nM), doses known to inhibit the ENaC, inhibit the myogenic vasoconstriction response to increasing perfusion pressure by blocking the activity of ENaC proteins. Amiloride completely inhibits Na+ influx in doses known to be relatively specific for ENaC (1.5 μM) in vascular smooth muscle cells (VSMC). [1]
In vivo Amiloride at 1 mg/kg/day subcutaneously is found to reverse the initial increases in collagen deposition and prevent any further increases in the DOCA-salt hypertensive rat. Amiloride delays the onset of proteinuria and improved brain and kidney histologic scores in the saline-drinking, stroke-prone spontaneously hypertensive rats (SHRSP). compared with controls. Amiloride antagonizes or prevents actions of aldosterone in these cells and in cardiovascular and renal tissues in animals with salt-dependent forms of hypertension. [1]
Features

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Teiwes J, et al. Am J Hypertens, 2007, 20(1), 109-117.

Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2015-06-27)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT01910259 Recruiting Secondary Progressive Multiple Sclerosis University College, London|Medical Research Council|Natio  ...more University College, London|Medical Research Council|National Institute for Health Research, United Kingdom|MS Society|University of Edinburgh|Queen Mary University of London|Keele University|University of Sheffield|University of Leeds|University of Warwick December 2014 Phase 2
NCT01879527 Recruiting Optic; Neuritis, With Demyelination Medical University of Vienna March 2014 Phase 2
NCT01918488 Enrolling by invitation Diabetic Nephropathies|Hypertension University of Southern Denmark|Odense University Hospital  ...more University of Southern Denmark|Odense University Hospital|Region Southern Denmark|Ministry of Science, Innovation and Higher Education (Denmark)|Danish Heart Foundation October 2013 --
NCT01804777 Terminated Proteinuria|Hypertension|Type II Diabetes University of New Mexico|Dialysis Clinic, Inc.|University  ...more University of New Mexico|Dialysis Clinic, Inc.|University of Pittsburgh March 2013 Phase 0
NCT01802489 Active, not recruiting Optic Neuritis|Multiple Sclerosis University of Oxford|Multiple Sclerosis Society of Great  ...more University of Oxford|Multiple Sclerosis Society of Great Britain and Northern Ireland February 2013 Phase 2

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Chemical Information

Download Amiloride HCl SDF
Molecular Weight (MW) 266.09
Formula

C6H8ClN7O.HCl

CAS No. 2016-88-8
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms N/A
Solubility (25°C) * In vitro DMSO 53 mg/mL (199.18 mM)
Water 6 mg/mL (22.54 mM)
Ethanol 5 mg/mL (18.79 mM)
In vivo
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name 1-(3,5-diamino-2-chloropyrazine-6-carbonyl)guanidine hydrochloride

Product Use Citation (1)

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