YM-58790

YM-58790CAS号: 168830-70-4分子式: C27H31N3O2分子量: 429.55描述纯度储存/保存方法靶点In vitro(体外研究)In vivo(体内研究)

产品描述
描述
YM-58790 free base is a potent mAChR antagonist.YM-58790 free base inhibited M1 mAChR, M2 mAChR, and M3 mAChR with Ki values of 28 nM, 260 nM, and 15 nM, respectively.YM-58790 free base inhibits reflex rhythmic bladder contraction in rats by inhibiting bladder pressurization. YM-58790 free base inhibits reflex rhythmic bladder contractions in rats by inhibiting bladder pressurization.
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.
生物活性
靶点
mAChR3:15 nM (Ki), mAChR2:260 nM (Ki), mAChR1:28 nM (Ki)
In vitro(体外研究)
YM-58790 free base (compound 18b) (0-1 μM) exerts a potent inhibitory effect on urinary bladder contraction while having minimal impact on bradycardia. In vitro, YM-58790 demonstrates selective antagonism between urinary bladder contraction and salivary secretion.[1]
In vivo(体内研究)
YM-58790 free base (3 mg/kg, i.v.) exhibits no impact on oxotremorine-induced tremor in mice.[1]
YM-58790 free base (6.0 mg/kg; i.v.) exhibits limited M1 and M2 antagonistic effects in vivo on McN-A343-induced pressor response in pithed rats. However, it demonstrates robust efficacy in M3 antagonism, with an ED30 value of 0.36 mg/kg and an ID50 value of 2.4 mg/kg.[1]
YM-58790 free base demonstrates robust inhibitory activity on bladder pressure during reflexly-evoked rhythmic contractions in rats.[1]