Amiloride HCl dihydrate

製品コードS2560 バッチS256001

化学情報

	Synonyms	MK-870 hydrochloride dihydrate	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₆H₈ClN₇O.HCl.2H₂O
	分子量	302.12	CAS No.	17440-83-4
Solubility (25°C)*	体外	DMSO	100 mg/mL (330.99 mM)
		Water	5 mg/mL warmed with 50ºC water bath (16.54 mM)
		Ethanol	0 mg/mL (0.0 mM)
* <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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	Amiloride HCl dihydrate(MK-870 hydrochloride dihydrate) is a potent epithelial sodium channel (ENaC) blocker, used in the management of hypertension and congestive heart failure.
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]

製品説明

Amiloride HCl dihydrate(MK-870 hydrochloride dihydrate) is a potent epithelial sodium channel (ENaC) blocker, used in the management of hypertension and congestive heart failure.

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]

プロトコル(参考用のみ)

参考

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長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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