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Catalog No. T16475Cas No. 459856-18-9
Pexacerfont (BMS-562086) is a selective antagonist of the corticotropin-releasing factor receptor (IC50: 6.1±0.6 nM for the human CRF1 receptor).
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Pack SizePrice/USDAvailabilityQuantity
1 mg$40In Stock
5 mg$89In Stock
1 mL x 10 mM (in DMSO)$98In Stock
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Product Introduction

Pexacerfont (BMS-562086) is a selective antagonist of the corticotropin-releasing factor receptor (IC50: 6.1±0.6 nM for the human CRF1 receptor).
In vitro
Pexacerfont shows an effective and specific inhibitory effect (IC50=6.1 ± 0.6 nM) toward the human CRF1 receptor. It also has greater than 1000-fold lower affinity (IC50>1000 nM) for the CRF-binding protein and biogenic amine receptors[1].
In vivo
Pexacerfont is active in rats (1-10 mg/kg, orally) in the defensive withdrawal and elevated plus-maze models of anxiety. The CLp of Pexacerfont was higher in rats (17.9 mL/kg per min) and dogs (11.6 mL/kg per min) than in chimpanzees (2.0 mL/kg per min). The plasma Pexacerfont concentrations exhibited a multiexponential decline in rats, dogs, and chimpanzees after the intravenous bolus dose. Assuming the value of CLp of Pexacerfont approximates the value of CLb in these three species, Pexacerfont has an estimated hepatic extraction ratio of 0.32, 0.38, and 0.08 in rats, dogs, and chimpanzees, respectively (calculated by dividing CLp by respective hepatic blood flow, 55.2, 30.9, and 25.5 mL/kg per min for rats, dogs, and chimpanzees). The assumption that CLb is equal to CLp is reasonable at least in rats, where the blood to the plasma concentration ratio of BMS-562086-equivalent radioactivity was 0.95 at 1 h postdose[1].
Chemical Properties
Molecular Weight340.42
Cas No.459856-18-9
Storage & Solubility Information
Storagestore at low temperature Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Solubility Information
DMSO: 45 mg/mL (132.2 mM)
Solution Preparation Table
1 mM2.9375 mL14.6877 mL29.3755 mL146.8774 mL
5 mM0.5875 mL2.9375 mL5.8751 mL29.3755 mL
10 mM0.2938 mL1.4688 mL2.9375 mL14.6877 mL
20 mM0.1469 mL0.7344 mL1.4688 mL7.3439 mL
50 mM0.0588 mL0.2938 mL0.5875 mL2.9375 mL
100 mM0.0294 mL0.1469 mL0.2938 mL1.4688 mL


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