|N-((R)-仲丁基)-8-(6-甲氧基-2-甲基吡啶-3-基)-2,7-二甲基吡唑并[1,5-a][1,3,5]三嗪-4-胺|CsnPharm

CAS No.: 459856-18-9

Pexacerfont Catalog No. CSN24468

Synonyms: BMS-562086;DPC-A69448;BMS-562,086

Pexacerfont is a potent and selective antagonist with IC50 value of 6.1nM.

规格	价格	促销价格	库存	数量

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

加入购物车大规格询价

加入收藏

产品咨询

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

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 V_z of pexacerfont in the rats, dogs, andchimpanzee was 14.9, 28.2, and 4.2 l/kg, respectively. The terminal plasma elimination t_1/2 values ranged from 13 to 43 h in rats, dogs, and chimpanzees. After oral administration, peak plasma concentrations (T_max) 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].
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

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.9375 mL
- 14.6876 mL
- 29.3752 mL
- 5 mM
- 0.5875 mL
- 2.9375 mL
- 5.8750 mL
- 10 mM
- 0.2938 mL
- 1.4688 mL
- 2.9375 mL

技术信息

CAS号

459856-18-9

储存条件

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

液体: -20°C:3-6 月 -80°C:12月

分子式

C18H24N6O

运输

蓝冰

分子量

340.42

别名

BMS-562086;DPC-A69448;BMS-562,086

溶解度

DMSO	95.0 mg/mL (279.1 mM) warming

动物实验配方

大规格询价

号为必填项

姓名: 邮箱: 手机号:

留言:

提交

Pexacerfont Catalog No. CSN24468

靶点选择性

请登录您的专属账户

确认信息