YM-58790

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

YM-58790 free base 是一种有效的 mAChR 拮抗剂。YM-58790 free base 结合 mAChR 亚型的 Ki 值分别为 28 nM (M1 mAChR)，260 nM (M2 mAChR)，和 15 nM (M3 mAChR)。YM-58790 free base 对大鼠的反射性节律性收缩膀胱加压有较强的抑制活性。

YM-58790 free base is a potent antagonist of mAChR. YM-58790 free base binds M1, M2, M3 with Ki values of 28 nM, 260 nM, and 15 nM. YM-58790 free base exhibits potent inhibitory activity on bladder pressuer in reflexly-evoked rhythmic contraction in rats.

YM-58790 free base (compound 18b) (0-1 μM) shows potent inhibitory effect on urinary bladder contraction, but has little effect on bradycardia. YM-58790 exhibits selective antagonism between urinary bladder contraction and salivary secretion in vitro.

YM-58790 free base (3 mg/kg, i.v.) has no effect on oxotremorine-induced tremor in mice. YM-58790 free base (6.0 mg/kg; i.v.) shows poor M1 and M2 antagonism effect in vivo on McN-A343-induced pressor in pithed rats, but displays potent efficacy on M3 antagonism with an ED30 value of 0.36 mg/kg (i.v.) and an ID50 value of 2.4 mg/kg (i.v.). YM-58790 free base exhibits potent inhibitory activity on bladder pressuer in reflexly-evoked rhythmic contraction, similar to Oxybutynin (HY-B0267), and has about ten times less inhibitory effect on oxotremorine-induced salivary secretion than oxybutynin in rats.

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Cell Cycle/DNA Damage

AChR

AChR

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168830-70-4

429.55

C27H31N3O2

>98% (HPLC)

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C(NC(OC1CCN(CC2=CC=C(NC)C=C2)CC1)=O)(C3=CC=CC=C3)C4=CC=CC=C4

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(-20℃)

With Ice Pack

≥ 2 years