ML193

生物活性靶点体外研究体内研究 ML193 试剂级价格

ML193

CAS号:713121-80-3
英文名:ML193
中文名:ML193
CBNumber:CB74199381
分子式:C28H25N5O4S
分子量:527.59
MOL File:713121-80-3.mol

ML193化学性质

储存条件 :Store at -20°C
溶解度 :≤0.1mg/ml in ethanol;2mg/ml in DMSO;3mg/ml in dimethyl formamide
形态 :crystalline solid
颜色 :Off-white to yellow

ML193性质、用途与生产工艺

生物活性 ML-193 (CID 1261822) 是一种有效和选择性的 GPR55 拮抗剂，IC50 值为 221 nM。ML-193 对 GPR55 的选择性是 GPR35，CB1 和 CB2 的 27 倍以上。ML-193 可以改善帕金森氏病 (PD) 大鼠的运动和感觉运动缺陷。
靶点

IC50: 221 nM (GPR55)
体外研究

ML-193 (0.01-100 μM; pretreated for 15 min) inhibits β-arrestin trafficking induced by L-α-lysophophosphatidylinositol (LPI, 10 μM) and ML186 (1 μM) with IC ₅₀ s of 0.22 μM and 0.12 μM, respectively.
ML-193 (0.01-10 μM; pretreated for 30 min) decreases the LPI-mediated ERK1/2 phosphorylation, with an IC ₅₀ of 0.2 μM in U2OS cells.
ML-193 (5 μM; pretreated for 30 min) attenuates the GPR55 agonists induced increases in hNSCs proliferation rates.
ML-193 (5 μM; 10 d) attenuates the ML184-induced increases in hNSCs differentiation.

体内研究

ML193 (1 and 5 µg/rat; intra-striatal at a rate of 1 μL/min) attenuates sensorimotor deficits and slip steps, increases motor coordination in PD rats.

Animal Model:	Male Wistar rats (200-250 g) were induced experimental Parkinson by 6-hydroxydopamine (6-OHDA, 10 µg/rat)
Dosage:	1 and 5 µg/rat
Administration:	Injected into the right striatum at a rate of 1 μL/min
Result:	Increased the time on the rotarod, decreased latency to remove the label and slip steps in 6-OHDA-lesioned rats.