Pexacerfont 是一种选择性的促肾上腺皮质激素释放因子 (CRF₁) 受体拮抗剂，作用于人 CRF₁ 受体，IC₅₀ 为 6.1±0.6 nM。

Pexacerfont is a selective corticotropin-releasing factor (CRF 1 ) receptor antagonist with IC 50 of 6.1±0.6 nM for human CRF 1 receptor.

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IC50: 6.1±0.6 nM (human CRF1 receptor)

Pexacerfont demonstrates a potent and specific inhibitory effect (IC50=6.1 ± 0.6 nM) toward human CRF1 receptor and has greater than 1000-fold lower affinity (IC50>1000 nM) for the CRF-binding protein and biogenic amine receptors. has not independently confirmed the accuracy of these methods. They are for reference only.

Pexacerfont (BMS-562086) is active in rats (1-10 mg/kg, orally) in the defensive withdrawal and elevated plus maze models of anxiety. After the intravenous bolus dose, the plasma Pexacerfont concentrations exhibited a multiexponential decline in rats, dogs, and chimpanzees. The CL p 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). Assuming the value of CL p of Pexacerfont approximates the value of CL b 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 CL p by respective hepatic blood flow, 55.2, 30.9, and 25.5 mL/kg per min for rats, dogs, and chimpanzees). The assumption that CL b is equal to CL p is reasonable at least in

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[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.

In Vitro: DMSO : 50 mg/mL (146.88 mM; Need ultrasonic)配制储备液