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Pexacerfont
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Pexacerfont图片
CAS NO:459856-18-9
包装与价格:
包装价格(元)
1 mg电议
5 mg电议
10 mg电议
100 mg电议
1 mL*10 mM(in DMSO)电议

产品名称
BMS-562086
产品介绍
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。

产品描述

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

体外活性

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].

体内活性

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].

Cas No.

459856-18-9

分子式

C18H24N6O

分子量

340.42

别名

BMS-562086

储存和溶解度

DMSO:45mg/mL (132.2mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years