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BMS-248360

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Catalog No. T14672Cas No. 254737-87-6

BMS-248360 is a potent, 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 receptors, respectively. BMS-248360 demonstrates hypertensive effects[1].

BMS-248360

BMS-248360

😃Good
Catalog No. T14672Cas No. 254737-87-6
BMS-248360 is a potent, 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 receptors, respectively. BMS-248360 demonstrates hypertensive effects[1].
Pack SizePriceAvailabilityQuantity
25 mg$2,72010-14 weeks
50 mg$3,58010-14 weeks
100 mg$4,90010-14 weeks
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Product Introduction

Bioactivity
Description
BMS-248360 is a potent, 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 receptors, respectively. BMS-248360 demonstrates hypertensive effects[1].
Targets&IC50
ETA receptor (rat):1.9 nM, AT1 (rat):6.0 nM(ki), ETA receptor (human):1.9 nM(ki), AT1 (human):(ki)10 nM
In vitro
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].
In vivo
BMS-248360 is orally bioavailable in rats (%F=38) with excellent oral exposure (Cmax=3.1 μM) and a reasonable elimination profile (T1/2=5.5 hours)[1]. At dosages of 30 and 100 μmol/kg (p.o.), it effectively blocks the hypertensive effects of intravenously administered AII[1].
Chemical Properties
Molecular Weight659.84
FormulaC36H45N5O5S
Cas No.254737-87-6
Relative Density.no data available
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

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