BMS-248360

Name: BMS-248360
Brand: TargetMol
SKU: T14672
Rating: 4.5 (1 reviews)

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产品编号 T14672Cas号 254737-87-6

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].

BMS-248360

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产品编号 T14672Cas号 254737-87-6

规格	价格	库存
25 mg	¥ 19,400	10-14周
50 mg	¥ 25,800	10-14周
100 mg	¥ 33,500	10-14周

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生物活性

产品描述	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].
靶点活性	ETA receptor (rat):1.9 nM, AT1 (rat):6.0 nM(ki), ETA receptor (human):1.9 nM(ki), AT1 (human):（ki）10 nM
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].