化合物YM-58790 T72038

Product Introduction
Bioactivity


英文名: YM-58790

描述: YM-58790 free base 是一种高效的 mAChR 拮抗剂。YM-58790 free base 对 M1 mAChR、M2 mAChR 和 M3 mAChR具有抑制作用， Ki 值分别为 28 nM ，260 nM ，和 15 nM 。YM-58790 free base 通过抑制膀胱加压来抑制大鼠的反射性节律性膀胱收缩。

体外活性: YM-58790 free base（0-1 μM）对尿道膀胱收缩具有强大的抑制效果，同时对心动过缓的影响极小。体外实验中，YM-58790表现出尿道膀胱收缩与唾液分泌之间的选择性拮抗作用。[1]

体内活性: 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]

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 60 mg/mL (139.68 mM)


关键字: YM-58790 | YM 58790 | YM58790

相关产品: 9-CP-Ade Mesylate | Anethole trithione | Dibucaine hydrochloride | 1,5-Diphenylpentan-1-one | Propantheline bromide | NS3861 | α-Conotoxin MII acetate | Cytisinicline | Primidone | Hupehenine

相关库: Anti-Neurodegenerative Disease Compound Library | Membrane Protein-targeted Compound Library | Bioactive Compounds Library Max | Bioactive Compound Library

化合物YM-58790 T72038信息由TargetMol中国为您提供，如您想了解更多关于化合物YM-58790 T72038报价、型号、参数等信息，欢迎来电或留言咨询。

注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途