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Pexacerfont

Catalog No. T16475 CAS 459856-18-9

Synonyms: BMS-562086

Pexacerfont 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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Pexacerfont, CAS 459856-18-9

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Purity: 98%

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Description	Pexacerfont is a selective antagonist of the corticotropin-releasing factor receptor (IC50: 6.1±0.6 nM for the human CRF1 receptor).
Targets&IC50	human CRF1 receptor:6.1±0.6 nM
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].

Synonyms	BMS-562086
Molecular Weight	340.42
Formula	C18H24N6O
CAS No.	459856-18-9

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 45mg/mL (132.2mM), Need ultrasonic

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

1. Zhou L, et al. In vitro and in vivo metabolism and pharmacokinetics of BMS-562086, a potent and orally bioavailable corticotropin-releasing factor-1 receptor antagonist. Drug Metab Dispos. 2012 Jun;40(6):1093-103.

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Keywords

Pexacerfont 459856-18-9 其他 Others BMS-562086 Inhibitor inhibitor inhibit

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