BMS-248360
CAS No. : 254737-87-6
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| Cat. No. : | HY-114953 |
| M.Wt: | 659.84 |
| Formula: | C36H45N5O5S |
| Purity: | >98 % |
| Solubility: | 10 mM in DMSO |
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].
IC50 & Target: Ki: 10 nM (hAT1), 1.9 nM (hETA receptor), 6.0 nM (rAT1), 1.9 nM(rETA receptor)[1]
In Vitro: 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].
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