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.
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纯度 |
98%
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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.
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基本信息 | |
别名 |
AZD7325
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可溶性/溶解性 |
DMSO : 250 mg/mL (705.46 mM; Need ultrasonic)
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生物活性 | |
靶点 |
CYP1A2;CYP3A4
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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.
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分子结构图