奥美沙坦作用机制 - Medchemexpress - MCE中国

1、Product Data SheetOlmesartanCat. No.: HY-17004CAS No.: 144689-24-7分式: CHNO分量: 446.5作靶点: Angiotensin Receptor作通路: GPCR/G Protein储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 50 mg/mL (111.98 mM; Need ultrasonic)SolventMass1 mg 5 mg 10 mgConcentration制备储备液1 mM

2、2.2396 mL 11.1982 mL 22.3964 mL5 mM 0.4479 mL 2.2396 mL 4.4793 mL10 mM 0.2240 mL 1.1198 mL 2.2396 mL请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存式和期限：-80C, 6 months; -20C, 1 month。-80C 储存时，请在 6 个内使，-20C 储存时，请在 1 个内使。体内实验请根据您的实验动物和给药式选择适当的溶解案。以下溶解案都请先按照 In Vitro 式配制澄清的储备液，再依次添加助溶剂：为保证实

3、验结果的可靠性，澄 的储备液可以根据储存条件，适当保存；体内实验的作液，建议您现现配，当天使； 以下溶剂前显的百分 指该溶剂在您配制终溶液中的体积占；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的式助溶1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (5.60 mM); Clear solution此案可获得 2.5 mg/mL (5.60 mM，饱和度未知) 的澄清溶液。以 1 mL 作液为例，取 100 L 25.0 mg/mL 的澄 DMSO 储备液加到 400 L P

4、EG300 中，混合均匀；向上述体系中加50 L Tween-80，混合均匀；然后继续加 450 L 理盐定容 1 mL。2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (5.60 mM); Clear solution此案可获得 2.5 mg/mL (5.60 mM，饱和度未知) 的澄清溶液。Page 1 of 2 www.MedChemE以 1 mL 作液为例，取 100 L 25.0 mg/mL 的澄均匀。DMSO 储备液加到 900 L 20% 的 SBE-CD 理盐溶液中，混合3. 请依序添

5、加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (5.60 mM); Clear solution此案可获得 2.5 mg/mL (5.60 mM，饱和度未知) 的澄 溶液，此案不适于实验周 期在半个以上的实验。以 1 mL 作液为例，取 100 L 25.0 mg/mL 的澄 DMSO 储备液加到 900 L 油中，混合均匀。BIOLOGICAL ACTIVITY物活性 Olmesartan (RNH-6270)管紧张素II受体 (AT1R) 拮抗剂，常于治疗压。体外研究 Olmesartan (0.7-5 mM; 24, 48 and 7

6、2 h) inhibits the growth of HeLa cells as a concentration- and time-dependentmode3.Cell Viability Assay3Cell Line: Human cervical cancer cell line (HeLa)Concentration: 0.7- 5 mMIncubation Time: 24, 48 and 72 hResult: IC50s against HeLa cell line are 4.685 and 1.651 mM for 48 and 72 h, respectively.体

7、内研究 Repeated dosing of olmesartan (1 mg/kg, 2 mg/kg, p.o.) dose-dependently decreases mean arterial blood pressure(MAP) in SHR without significant influence on body weight and food intake during 10 weeks1. Olmesartan (5 mg/kg/d, p.o.) and Hyd treatments lower systolic blood pressure to the same degr

8、ee in mice. Olmesartan treatmentinhibits cardiac hypertrophy, evaluated by echocardiography, heart weight, cross-sectional area of cardiomyocytes,and gene expression. Olmesartan treatment reverses decreased gene expressions of ACE2 and Mas receptor of Ren-Tg mice and inhibits enhanced NADPH oxidase

9、(Nox)4 expression and reactive oxygen species2.户使本产品发表的科研献 Sleep. 2018 Mar 1;41(3). Biomed Pharmacother. 2017 Sep;93:429-434. J Physiol Sci. 2018 Mar;68(2):153-164. Int J Biochem Cell Biol. 2020 Jan 31;121:105703. J Lumin. 2018 Nov; 203;616-628.See more customer validations on HYPERLINK www.MedChemE

10、 www.MedChemEREFERENCES1. Yanagihara H, et al. Effects of telmisartan and olmesartan on insulin sensitivity and renal function in spontaneously hypertensive rats fed a high fat diet. JPharmacol Sci. 2016 Jul;131(3):190-7.2. Tanno T, et al. Olmesartan Inhibits Cardiac Hypertrophy in Mice Overexpressi

11、ng Renin Independently of Blood Pressure: Its Beneficial Effects onPage 2 of 3 www.MedChemEACE2/Ang(1-7)/Mas Axis and NADPH Oxidase Expression. J Cardiovasc Pharmacol. 2016 Jun;67(6):503-9.3. Bakhtiari E, et al. Synergistic, cytotoxic and apoptotic activities of olmesartan with NF-B inhibitor against HeLa human cell line. Toxicol Mech Methods.2015;25(8):614-21.McePdfHeightCaution: Product has not been fully valida