ML-193 是一种有效的选择性GPR55拮抗剂,IC50值为 221 nM,对 GPR55 的选择性比 GPR35、CB1 和 CB2 高 27 倍以上,可改善帕金森病 (PD) 大鼠的运动和感觉运动缺陷。
产品描述
ML-193 is a potent and selective GPR55 antagonist( IC50 : 221 nM). It shows more than 27-fold selectivity for GPR55 over GPR35, CB1 and CB2, and can improve the motor and the sensorimotor deficits of Parkinson’s disease (PD) rats.
体外活性
ML193, a selective GPR55 antagonist.?ML184 significantly promoted neuronal differentiation in vitro while ML193 reduced differentiation rates as compared to vehicle treatment.Continuous administration of O-1602 into the hippocampus via a cannula connected to an osmotic pump resulted in increased Ki67+ cells within the dentate gyrus.?O-1602 increased immature neuron generation, as assessed by DCX+ and BrdU+ cells, as compared to vehicle-treated animals.?GPR55-/- animals displayed reduced rates of proliferation and neurogenesis within the hippocampus while O-1602 had no effect as compared to vehicle controls[2].
体内活性
Intra-striatal administration of ML193 increased time on the rotarod, decreased latency to remove the label and slip steps in 6-OHDA-lesioned rats mostly at the dose of 1 g/rat[1].
Cas No.
713121-80-3
分子式
C28H25N5O4S
分子量
527.6
别名
CID 1261822
储存和溶解度
DMSO:60 mg/ml (113.72 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years