Amiloride HCl

Catalog No.S1811

Amiloride HCl  Chemical Structure

Molecular Weight(MW): 266.09

Amiloride is a selective T-type calcium channel blocker, an epithelial sodium channel blocker and a selective inhibitor of urokinase plasminogen activator (uPA)(Ki=7 μM).

Size Price Stock Quantity  
In DMSO USD 130 In stock
USD 97 In stock
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Biological Activity

Description Amiloride is a selective T-type calcium channel blocker, an epithelial sodium channel blocker and a selective inhibitor of urokinase plasminogen activator (uPA)(Ki=7 μM).
Targets
Sodium channel [1] T-type calcium channel [2] uPA [3]
7 μM(Ki)
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]

Protocol

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 Information

Molecular Weight 266.09
Formula

C6H8ClN7O.HCl

CAS No. 2016-88-8
Storage powder
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03031496 Not yet recruiting Hypertension GlaxoSmithKline March 2017 Phase 1
NCT02847338 Not yet recruiting Hypertension Cambridge University Hospitals NHS Foundation Trust|Medical Research Council November 2016 Phase 4
NCT02875886 Not yet recruiting Chronic Kidney Disease Erasmus Medical Center September 2016 Phase 4
NCT02525796 Recruiting Primary Hyperparathyroidism Brigham and Womens Hospital January 2016 Phase 2|Phase 3
NCT02832973 Recruiting Hypertension Resistant to Conventional Therapy Sao Jose do Rio Preto University September 2015 Phase 4
NCT02896621 Recruiting Hypertension|Sleep Apnea Hospital de Clinicas de Porto Alegre April 2015 Phase 3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID