化合物 T14672 T14672

Product Introduction
Bioactivity


英文名: BMS-248360

描述: BMS-248360 is a potent and orally active dual antagonist of both angiotensin II receptor (AT1) and endothelin A (ETA) receptor. With Kis of 10 nM and 1.9 nM for hAT1 and hETA receptor, respectively. BMS-248360 shows hypertensive effects[1].

体外活性: BMS-248360 shows no activity against AT2 and ETB receptor subtypes and it also shows activity against rat AT1 and rat ETA receptor, with Kis of 6.0 nM and 1.9 nM, respectively[1].

体内活性: BMS-248360 is found to be orally bioavailable in rats (%F=38). It has excellent oral exposure (Cmax)=3.1 μM) and reasonable elimination profile (T1/2=5.5 hours)[1]. BMS-248360 (30 μmol/kg, 100 μmol/kg; p.o.) blocks the hypertensive effects of intravenously administered AII[1].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

关键字: BMS-248360 | BMS 248360 | BMS248360

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