Amiloride HCl dihydrate
Catalog No.S2560
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.
Cited by 1 publication
Purity & Quality Control
Choose Selective Sodium Channel Inhibitors
Biological Activity
| Description | 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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| Targets |
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| In vitro |
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. [1] Amiloride precludes the alkalinization and in parallel inhibit cellular proliferation. Amiloride directly inhibits autophosphorylation of the EGF receptor. [2] Amiloride significantly enhances recovery to a maximum of 39%, 88%, and 78% for force, +dF/dt, and -dF/dt, respectively. [3] 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. [4] 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. [5] |
Protocol
Solubility (25°C)
| In vitro | DMSO | 60 mg/mL (198.59 mM) |
|---|---|---|
| Water | 17 mg/mL (56.26 mM) | |
| Ethanol | 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 | 302.12 |
|---|---|
| Formula | C6H8ClN7O.HCl.2H2O |
| CAS No. | 17440-83-4 |
| Storage | powder |
| Synonyms | N/A |
Bio Calculators
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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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