产品
编 号：F715561
分子式：C36H45N5O5S
分子量：659.84
分子式：C36H45N5O5S
分子量：659.84
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CAS No: 254737-87-6
产品详情
生物活性：
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 displays hypertensive effects.
体内研究：
BMS-248360 is found to be orally bioavailable in rats (%F=38) with excellent oral exposure (Cmax)=3.1 μM) and reasonable elimination profile (T1/2=5.5 hours).BMS-248360 (30 μmol/kg, 100 μmol/kg; p.o.) blocks the hypertensive effects of intravenously administered AII.Animal Model:Male Rats
Dosage:30 μM/kg, 100 μM/kg
Administration:Oral administration
Result:Blocked the hypertensive effects of intravenously administered AII.
Animal Model:Male Rats
Dosage:10 μM/kg
Administration:Oral administration
Result:T1/2= 5.5 hours
体外研究：
BMS-248360 shows activity against rat AT1 and rat ETA receptor, with Kis of 6.0 nM and 1.9 nM, respectively.BMS-248360 shows no activity against AT2 and ETB receptor subtypes.
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 displays hypertensive effects.
体内研究：
BMS-248360 is found to be orally bioavailable in rats (%F=38) with excellent oral exposure (Cmax)=3.1 μM) and reasonable elimination profile (T1/2=5.5 hours).BMS-248360 (30 μmol/kg, 100 μmol/kg; p.o.) blocks the hypertensive effects of intravenously administered AII.Animal Model:Male Rats
Dosage:30 μM/kg, 100 μM/kg
Administration:Oral administration
Result:Blocked the hypertensive effects of intravenously administered AII.
Animal Model:Male Rats
Dosage:10 μM/kg
Administration:Oral administration
Result:T1/2= 5.5 hours
体外研究：
BMS-248360 shows activity against rat AT1 and rat ETA receptor, with Kis of 6.0 nM and 1.9 nM, respectively.BMS-248360 shows no activity against AT2 and ETB receptor subtypes.
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