BMS-248360 

BMS-248360 is a potent and orally active dual antagonist of both angiotensin II receptor (AT1) and endothelin A (ET_A) receptor, with K_is of 10 nM and 1.9 nM for hAT1 and hETA receptor, respectively. BMS-248360 displays hypertensive effects^[1].

Ki: 10 nM (hAT1), 1.9 nM (hETA receptor), 6.0 nM (rAT1), 1.9 nM(rET_A receptor)^[1]

BMS-248360 shows activity against rat AT1 and rat ET_A receptor, with K_is of 6.0 nM and 1.9 nM, respectively^[1].
BMS-248360 shows no activity against AT2 and ET_B receptor subtypes^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

BMS-248360 is found to be orally bioavailable in rats (%F=38) with excellent oral exposure (C_max)=3.1 µM) and reasonable elimination profile (T_1/2=5.5 hours)^[1].
BMS-248360 (30 µmol/kg, 100 µmol/kg; p.o.) blocks the hypertensive effects of intravenously administered AII^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

659.84

C₃₆H₄₅N₅O₅S

254737-87-6

O=S(C1=CC=CC=C1C2=CC=C(CN3C(CCCC)=NC4(CCCC4)C3=O)C=C2CN5C(C(C)(C)CC5)=O)(NC6=C(C)C(C)=NO6)=O

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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.  [Content Brief]