Amiloride HCl dihydrate
Molecular Weight(MW): 302.12
Amiloride HCl dihydrate is a potent epithelial sodium channel (ENaC) blocker, used in the management of hypertension and congestive heart failure.
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|Description||Amiloride HCl dihydrate is a potent epithelial sodium channel (ENaC) blocker, used in the management of hypertension and congestive heart failure.|
Amiloride also induces the dephosphorylation of P13K (phosphatidylinositol 3-kinase) and PDK-1 (phosphoinositide-dependent kinase-1) kinases along with PTEN (phosphatase and tensin homolog deleted on chromosome 10) and PP1 alpha phosphatases. Amiloride inhibits phosphorylation of kinases and phosphatases by competing with ATP. Amiloride, which causes little or no cytotoxicity by itself, enhances TRAIL-induced apoptosis.  Amiloride precludes the alkalinization and in parallel inhibit cellular proliferation. Amiloride directly inhibits autophosphorylation of the EGF receptor.  Amiloride significantly enhances recovery to a maximum of 39%, 88%, and 78% for force, +dF/dt, and -dF/dt, respectively.  Amiloride, a frequently used inhibitor of Na+/H+ exchange, rapidly inhibits phorbol ester-stimulated protein phosphorylation in vivo and protein kinase C-mediated phosphorylation in vitro, both with potency similar to that with which Amiloride inhibits Na+/H+ exchange. Amiloride blocks phorbol ester-induced adhesion of HL-60 cells (adhesion being a property indicative of the differentiated state), but dimethylamiloride (as well as ethylisopropylamiloride, another very potent amiloride analog) does not.  Amiloride inhibits the ouabain-sensitive rate of oxygen consumption (QO2) of a suspension of rabbit intact proximal tubules in the presence of different concentrations of extracellular sodium. 
-  Kim KM, et al. Oncogene,?005, 24(3), 355-366.
-  Koivusalo M, et al. J Cell Biol,?010, 188(4), 547-563.
-  Karmazyn M, et al. Am J Physiol,?988, 255(3 Pt 2), H608-615.
|In vitro||Water||17 mg/mL (56.26 mM)|
|DMSO||0 mg/mL (0.0 mM)|
|Ethanol||0 mg/mL (0.0 mM)|
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02323100||Recruiting||Drug: Ravicti low dose|Drug: Ravicti high dose|Drug: Placebo||Cystic Fibrosis||National Jewish Health|University of Alabama at Birmingham|Children''s Hospital of Philadelphia|Johns Hopkins University|Horizon Pharma Ireland Ltd. Dublin Ireland||December 2 2018||Phase 1|Phase 2|
|NCT02586883||Recruiting||Other: bronchial ddp test||Idiopathic Dilation of the Bronchi||Assistance Publique - Hôpitaux de Paris||March 29 2016||Not Applicable|
|NCT02325362||Completed||Drug: Miglustat ; placebo|Drug: Placebo ; Miglustat||Cystic Fibrosis||Assistance Publique - Hôpitaux de Paris|Actelion|CRCM (Centres de Ressources et de Compétences de la Mucoviscidose)||March 17 2015||Phase 2|Phase 3|
|NCT01918488||Unknown status||Dietary Supplement: Standardized salt diet|Drug: Amiloride||Diabetic Nephropathies|Hypertension||University of Southern Denmark|Odense University Hospital|Region of Southern Denmark|The Ministry of Science Technology and Innovation Denmark|Danish Heart Foundation||October 2013||Not Applicable|
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.
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