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.

Price Stock Quantity  
In DMSO USD 130 In stock
USD 97 In stock
Bulk Inquiry

Massive Discount Available

Free Overnight Delivery on all orders over $ 500.

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

  • Compare Sodium Channel Chemicals
    Compare Sodium Channel Products
  • Research Area

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]

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

SpeciesBaboonDogMonkeyRabbitGuinea pigRatHamsterMouse
Weight (kg)121031.
Body Surface Area (m2)
Km factor202012128653
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] Teiwes J, et al. Am J Hypertens, 2007, 20(1), 109-117.

Clinical Trial Information( data from, updated on 2015-03-23)

NCT Number Recruitment Conditions Sponsor
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 Acute Autoimmune Optic Neuritis 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 --
NCT01896661 Not yet recruiting Hypertension|Obstructive Sleep Apnea Hospital de Clinicas de Porto Alegre August 2013 Phase 3
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

view more

Chemical Information

Download Amiloride HCl SDF
Molecular Weight (MW) 266.09


CAS No. 2016-88-8
Storage 3 years -20℃Powder
6 months-80℃in solvent (DMSO, water, etc.)
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

Research Area

Product Use Citation (1)

Tech Support & FAQs

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

* Indicates a Required Field

Related Sodium Channel Products

  • Digoxin

    Digoxin is a sodium-potassium pump inhibitor, used in the treatment of atrial fibrillation and heart failure.

  • Procainamide HCl

    Procainamide HCl is a sodium channel blocker, and also a DNA methyltransferase inhibitor, used in the treatment of cardiac arrhythmias.

  • BTB06584

    BTB06584 is an IF1-dependent, selective inhibitor of the mitochondrial F1 Fo-ATPase.

  • Ouabain

    Ouabain is a selective Na+/K+, -ATPase inhibitor, binds to α2 /α3 subunit with Ki of 41 nM/15 nM.

    Features:A glycoside poison that binds to and inhibits the action of the Na+/K+ pump in the cell membrane.

  • A-803467

    A-803467 is a selective NaV1.8 channel blocker with IC50 of 8 nM, blocks tetrodotoxin-resistant currents, exhibits >100-fold selectivity against human NaV1.2, NaV1.3, NaV1.5, and NaV1.7.

    Features:The 1st small-molecule blocker of sodium channels showing both high potency and significant subtype-selectivity among the sodium channel family.

  • Rufinamide

    Rufinamide is a voltage-gated sodium channel blocker, used an anticonvulsant medication.

  • Phenytoin

    Phenytoin is an inactive voltage-gated sodium channel stabilizer.

  • Zonisamide

    Zonisamide is a sulfonamide anticonvulsant approved for use as an adjunctive.

  • Riluzole

    Riluzole is a drug used to treat amyotrophic lateral sclerosis.

  • Carbamazepine

    Carbamazepine (Carbatrol) is a sodium channel blocker with IC50 of 131 μM in rat brain synaptosomes.

    Features:Frequently prescribed first-line drug for the treatment of partial and generalized tonic-clonic epileptic seizures.

Recently Viewed Items

Tags: buy Amiloride HCl | Amiloride HCl ic50 | Amiloride HCl price | Amiloride HCl cost | Amiloride HCl solubility dmso | Amiloride HCl purchase | Amiloride HCl manufacturer | Amiloride HCl research buy | Amiloride HCl order | Amiloride HCl mouse | Amiloride HCl chemical structure | Amiloride HCl mw | Amiloride HCl molecular weight | Amiloride HCl datasheet | Amiloride HCl supplier | Amiloride HCl in vitro | Amiloride HCl cell line | Amiloride HCl concentration | Amiloride HCl nmr
Contact Us