YM-58790 (C09-1185-574)

YM-58790 is a potent antagonist of mAChR . YM-58790 binds M1 , M2 , M3 with K i values of 28 nM, 260 nM, and 15 nM. YM-58790 exhibits potent inhibitory activity on bladder pressuer in reflexly-evoked rhythmic contraction in ratsIn VitroYM-58790 (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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.In VivoYM-58790 (3 mg/kg, i.v.) has no effect on oxotremorine-induced tremor in mice . YM-58790 (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 ED 30 value of 0.36 mg/kg (i.v.) and an ID 50 value of 2.4 mg/kg (i.v.) . YM-58790 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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only.Form:SolidIC50& Target:mAChR3 15 nM (Ki) mAChR1 28 nM (Ki) mAChR2 260 nM (Ki). Specifications and Purity: 98%. Molecular Formula: C27H32ClN3O2. Molecular Weight: 466.01. PubChem CID: 129010504.