product name Amiloride HCl dihydrate
Description: Amiloride HCl dihydrate is a potent epithelial sodium channel (ENaC) blocker. Amiloride was first approved in 1967 (then known as MK 870), for in the management of hypertension and congestive heart failure. Amiloride works by directly blocking the epithelial sodium channel (ENaC) thereby inhibiting sodium reabsorption in the late distal convoluted tubules, connecting tubules, and collecting ducts in the kidneys (this mechanism is the same for triamterene). This promotes the loss of sodium and water from the body, but without depleting potassium.
References: Oncogene. 2005 Jan 13;24(3):355-66; J Cell Biol. 2010 Feb 22;188(4):547-63.
302.12
Formula
C6H8ClN7O.HCl.2H2O
CAS No.
17440-83-4
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 60 mg/mL (198.6 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
Synonyms
other peoduct :
| In Vitro |
In vitro activity: 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. Kinase Assay: Cell Assay: |
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| References | Oncogene. 2005 Jan 13;24(3):355-66; J Cell Biol. 2010 Feb 22;188(4):547-63. |
