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1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEAmiloride hydrochloride dihydrateCat. No.: HY-B0285BCAS No.: 17440-83-4Synonyms: MK-870 hydrochloride dihydrate分式: CHClNO分量: 302.12作靶點(diǎn): Sodium Channel作通路: Membrane Transporter/Ion Channel儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solv

2、ent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 100 mg/mL (330.99 mM; Need ultrasonic and warming)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 3.3099 mL 16.5497 mL 33.0994 mL5 mM 0.6620 mL 3.3099 mL 6.6199 mL10 mM 0.3310 mL 1.6550 mL 3.3099 mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度,選擇合適的溶劑配制儲(chǔ)備液,并請(qǐng)注意儲(chǔ)備液的保存式和期限。BIOLOGICA

3、L ACTIVITY物活性 Amiloride hydrochloride dihydrate上鈉通道 (ENaC) 和尿激酶型纖溶酶原激活物受體 (uTPA) 的抑制劑。IC50 & Target ENaC 1, uTPA 2體內(nèi)研究Amiloride hydrochloride dihydrate is a potent epithelial sodium channels (ENaCs) blocker. Amiloride is highlyconcentrated in the plasma 15 to 30 minutes following the injections. 2 m

4、g/kg dose of Amiloride1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEhydrochloride dihydrate has no effect on blood pressure, heart rate, mesenteric vascular resistance, orhindquarters vascular resistance as compare to the baseline measurements (n=7). Over a 2 hour period,Amiloride hydrochloride d

5、ihydrate elicits negligible responses in arterial pressure (-11 mmHg) and heart rate(-106 bpm/min) as compare to baseline levels. Results show an Amiloride hydrochloride dihydrate dose-related response pattern for the c-Fos activation in the area postrema (AP). Even at the lowest dose ofAmiloride hy

6、drochloride dihydrate (0.1 mg/kg), the number of c-Fos labeled neurons in the AP is statisticallydifferent from the control rats at a p 1.PROTOCOLAnimal The experiments are performed on male and female Sprague-Dawley rats that have been maintained in aAdministration 1 heat controlled room maintained

7、 at 23 C with a 12h/12h light-dark schedule. A total of 116 adult rats areinjected i.p. with Amiloride hydrochloride dihydrate (0.1, 0.5, and 2.0 mg/kg). After 15, 30, 45, or 120 minpost-injection, the rats are anesthetized with 8% chloral hydrate, the chest is opened, and blood samples areobtained

8、by cardiac puncture. The blood is centrifuged at 5000 RPM for 5 min, and the plasma (1.5 mL)separated and stored at -80 C 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.戶使本產(chǎn)品發(fā)表的科研獻(xiàn) J Am Chem Soc. 2018 Dec 12;140(49):17234-17240. Theranostics. 2019 Ma

9、y 31;9(13):3732-3753. Cell Physiol Biochem. 2018;51(6):2564-2574. Nanotechnology. 2018 Feb 23;29(8):085101. Microb Pathog. 2019 Jul 18:103638.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Miller RL, et al. Blockade of ENaCs by amiloride induces c-Fos activation of the area postrema. Brain Res. 2015 Mar 19;1601:40-51.2. Xu LB, et al. Amiloride, a urokinase-type plasminogen activator receptor (uTPA) inhibitor, reduces proteinurea in podocytes. Genet MolRes. 2015 Aug 14;14(3):9518-29.McePdfHeightCaution: Product has not been fully validate

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