AZD-7325

AZD-7325CAS号: 942437-37-8分子式: C19H19FN4O2分子量: 354.38描述纯度储存/保存方法别名可溶性/溶解性靶点In vitro(体外研究)In vivo(体内研究)

产品描述
描述
AZD-7325 is a potent and orally active partial selective PAM of GABAAα2 and Aα3 receptor (Ki=0.3 and 1.3 nM, respectively), and has less antagonistic efficacy at the Aα1 and Aα5 receptor subtypes. AZD-7325 is a moderate CYP1A2 and a potent CYP3A4 inducer in vitro. AZD-7325 has the potential for the investigation of anxiety and dravet syndrome.
纯度
98%
储存/保存方法
Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
基本信息
别名
AZD7325
可溶性/溶解性
DMSO : 250 mg/mL (705.46 mM; Need ultrasonic)
生物活性
靶点
CYP1A2;CYP3A4
In vitro(体外研究)
AZD-7325 is a high affinity and selective modulator of the GABAA receptor system, exhibits high binding affinity at GABAAα1, α2 and α3 (Ki=0.5, 0.3, and 1.3 nM, respectively), and low at GABAAα5 (Ki=230 nM).
AZD-7325 (0-10 µM; 3 consecutive days; once daily) causes a maximal CYP1A2 mRNA expression of 3.2-fold, 2.1-fold, and 2.5-fold in human hepatocytes from donor HH210, HH215, and HH216, respectively.
In vivo(体内研究)
AZD-7325 (oral administration; 10, 17.8 or 31.6 mg/kg; 30 minutes before the induction of hyperthermia) attenuates hyperthermia-induced seizures, shows median thresholds in the treatment groups of 42.8°C for 10 mg/kg, 43.3°C for 17.8 mg/kg, and 43.4°C for 31.6 mg/kg compares to 42.2°C in vehicle group.

分子结构图

AZD-7325