Revefenacin 是一种mAChR拮抗剂,在M3受体上具有高亲和力,Ki值为 0.18 nM。
产品描述
Revefenacin is a mAChR antagonist has a high affinity on M3 receptor( Ki : 0.18 nM),and potentially useful for the treatment of respiratory disease.
体内活性
In anesthetized dogs, TD-4208, along with tiotropium and glycopyrronium, produced sustained inhibition of acetylcholine-induced bronchoconstriction for up to 24 hours. In anesthetized rats, inhaled TD-4208 exhibited dose-dependent 24-hour bronchoprotection against methacholine-induced bronchoconstriction. The estimated 24-hour potency (expressed as concentration of dosing solution) was 45.0 μg/ml[1].
Cas No.
864750-70-9
分子式
C35H43N5O4
分子量
597.76
别名
GSK1160724;TD-4208;Revefenacin
储存和溶解度
DMSO:125 mg/mL (209.12 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years