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ML-193
GPR55拮抗剂,ML193(CID 1261822)是一种有效的选择性GPR55拮抗剂,IC50为221 nM,对GPR55的选择性分别比CB1,GPR35和CB2高>27倍,>145倍和>145倍;减少体外神经元分化,增加焦虑样行为,同时以0.1和1μg/大鼠的剂量通过i.c.v.注射引起运动损伤。
目录号: PC11472 纯度: ≥98%
CAS No. :713121-80-3
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中文名称
ML-193
中文别名
ML 193
英文名称
ML-193
英文别名
ML 193;ML-193
Cas No.
713121-80-3
分子式
C28H25N5O4S
分子量
527.59
包装储存
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
生物活性

ML-193 (CID 1261822) is a potent and selective antagonist of GPR55, with an IC50 of 221 nM. ML-193 shows more than 27-fold selectivity for GPR55 over GPR35, CB1 and CB2. ML-193 can improve the motor and the sensorimotor deficits of Parkinson’s disease (PD) rats.

性状

Solid

IC50 & Target[1][2]

IC50: 221 nM (GPR55)

体外研究(In Vitro)

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 IC50s 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 IC50 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.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

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.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

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.
运输条件

Room temperature or refrigerated transportation.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
参考文献
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