BMS-248360_product_DataBase

Bioactivity	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[1].
Target	Ki: 10 nM (hAT1), 1.9 nM (hETA receptor), 6.0 nM (rAT1), 1.9 nM(rETA receptor)
Invitro	BMS-248360 shows activity against rat AT1 and rat ETA receptor, with Kis of 6.0 nM and 1.9 nM, respectively[1].BMS-248360 shows no activity against AT2 and ETB receptor subtypes[1].
In Vivo	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)[1].BMS-248360 (30 µmol/kg, 100 µmol/kg; p.o.) blocks the hypertensive effects of intravenously administered AII[1]. Animal Model:
Name	BMS-248360
CAS	254737-87-6
Formula	C36H45N5O5S
Molar Mass	659.84
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[1]. Murugesan N, et al. Discovery of N-isoxazolyl biphenylsulfonamides as potent dual angiotensin II and endothelin A receptor antagonists. J Med Chem. 2002 Aug 29;45(18):3829-35.

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