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Pexacerfont

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Chemical Structure| 459856-18-9 同义名 : BMS-562086;DPC-A69448
CAS号 : 459856-18-9
货号 : A1166938
分子式 : C18H24N6O
纯度 : 99%+
分子量 : 340.423
MDL号 : MFCD22628864
存储条件：

粉末 Keep in dark place,Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(146.88 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 Corticotropin-releasing factor subtype 1 (CRF1) receptor mediates stress-induced activation of the hypothalamic-pituitary-adrenal axis. Pexacerfont is a selective antagonist of CRF1 receptor with IC50 of 6.1 ± 0.6 nM for human CRF1 receptor. Pexacerfont was orally bioavailable in rats, dogs, and chimpanzees, with an absolute oral bioavailability of 40.1, 58.8, and 58.5%, respectively. Pexacerfont had an estimated hepaticextraction ratio of 0.32, 0.38, and 0.08 in rats, dogs, and chimpanzees, respectively. The average Vz of pexacerfont in the rats, dogs, andchimpanzee was 14.9, 28.2, and 4.2 l/kg, respectively. The terminal plasma elimination t1/2 values ranged from 13 to 43 h in rats, dogs, and chimpanzees. After oral administration, peak plasma concentrations (Tmax) of pexacerfont were achieved in less than 2 h for all three species, indicating a rapid oral absorption. Virtual clinical trials performed with a population-based ADME simulator suggested that a minimal dose of 100 mg daily would provide sufficient drug exposure to achieve plasma concentrations above the projected human efficacious plasma concentration of pexacerfont (> 500 nM)[1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.94mL

0.59mL

0.29mL

14.69mL

2.94mL

1.47mL

29.38mL

5.88mL

2.94mL
参考文献

[1]Zhou L, Dockens RC, Liu-Kreyche P, Grossman SJ, Iyer RA. 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;40(6):1093-1103