Tasosartan-WAY-ANA-756-DataSheet-生命科學(xué)試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemETasosartanCat. No.: HY-A0250CAS No.: 145733-36-4Synonyms: WAY-ANA 756分式: CHNO分量: 411.46作靶點: Angiotensin Receptor作通路: GPCR/G Protein儲存式: Powder -20C 3 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 DMSO : 125 mg/mL (303.80 mM

2、; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 2.4304 mL 12.1518 mL 24.3037 mL5 mM 0.4861 mL 2.4304 mL 4.8607 mL10 mM 0.2430 mL 1.2152 mL 2.4304 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。體內(nèi)實驗 請根據(jù)您的實驗動物和給藥式選擇適當(dāng)?shù)娜芙獍?，配制前請先配制澄清的儲備液，再依次添加助溶?為保證實驗結(jié)果的可靠性，體內(nèi)實驗的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使；澄清的儲備液

3、可以根據(jù)儲存條件，適當(dāng)保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.08 mg/mL (5.06 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.08 mg/mL (5.06 mM); Clear solution3. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.08 mg/mL

4、(5.06 mM); Clear solution1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEBIOLOGICAL ACTIVITY物活性 Tasosartan種長效的管緊張素 II (AngII) 受體拮抗劑。IC50 & Target Angiotensin II (AngII) receptor 1體外研究 Tasosartan is an orally active nonpeptide AngII antagonist that has demonstrates specific and selective AT1receptor

5、 antagonistic activity in vitro. IC50 for inhibition of specific binding of 125I-AngII to rat adrenalmembrane in the absence of proteins in binding buffer is 1.20.6 nM 1.體內(nèi)研究 Administration of Tasosartan at doses of 1.0 and 3.0 mg/kg (iv) significantly (p 2.PROTOCOLAnimal Rats 2Administration 2 Pres

6、sor response to angiotensin-II administration in four groups of rats (n=3-5 each, weighing 3438 g).Each rat is subjected to four separate bolus injections of angiotensin-II following the introduction of either thevehicle or graded doses of Tasosartan (0.3, 1.0, or 3.0 mg/kg, iv) 2.MCE has not indepe

7、ndently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Maillard MP, et al. Tasosartan, enoltasosartan, and angiotensin II receptor blockade: the confounding role of protein binding. JPharmacol Exp Ther. 2000 Nov;295(2):649-54.2. Elokdah HM, et al. Novel human metabolites of the angiotensin-II antagonist Tasosartan and their pharmacological effects. Bioorg MedChem Lett. 2002 Aug 5;12(15):1967-71.McePdfHeightCaution: Product has not been fully validated for medical applications.For res