ML-193 (Synonyms:CID 1261822)
目录号 : KM8208 CAS No. : 713121-80-3

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。

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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.

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 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.

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.
分子式
C28H25N5O4S
分子量
527.59
CAS号
713121-80-3
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

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