CHF5407

CHF5407CAS号: 1004312-94-0分子式: C27H25BrF4N2O3S分子量: 613.46描述储存/保存方法In vitro(体外研究)In vivo(体内研究)

产品描述
描述
CHF5407(SVT-47060) is a potent and selective muscarinic M3 receptor antagonist with prolonged action at muscarinic receptors.CHF5407 has an effect on bronchospasm and may be used in the study of respiratory disorders.CHF5407 is a potent and selective muscarinic M3 receptor antagonist with prolonged action at muscarinic receptors.
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.
生物活性
In vitro(体外研究)
Producing a potent (pIC50=9.0-9.6) and long-lasting (up to 24 h) inhibition of M3 receptor-mediated contractile responses to carbachol in the guinea pig isolated trachea and human isolated bronchus, CHF5407 exhibits a very slow dissociation from M3 receptors (hM3; t1/2=166 min) and markedly short-acting effects at M2 receptors (hM2; t1/2=31 min)[1].
In vivo(体内研究)
Administered intratracheally in a single dose of 100 μl at doses of 0.1, 0.3, and 1 nmol/kg, CHF5407 exerted a dose-dependent and potent inhibition of ACh-induced bronchospasm (20 g/kg; i.v.) in guinea pigs (450-550 g), with an ED50 value of 0.15 nmol/kg[1].