|N-(4-(N-(3,4-二甲基异恶唑-5-基)氨磺酰基)苯基)-6,8-二甲基-2-(吡啶-2-基)喹啉-4-甲酰胺|CsnPharm

CAS No.: 713121-80-3

ML-193 Catalog No. CSN22976

Synonyms: CID 1261822

ML 193 is a selective GPR55 antagonist with IC50 of 221 nM.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述G protein-coupled receptor 55 (GPR55) belongs to the class A family of G-protein coupled receptor (GPCRs)^[1]. GPR55 was activated by a range of plant, synthetic and endogenous cannabinoids and blocked by the non-psychoactive phytocannabinoid, cannabidiol. 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. 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^[2]. M184 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^[3].
临床研究
NCT号适应症或疾病临床期招募状态预计完成时间地点
NCT01500278 - - Completed - -
NCT01500278 Rheumatoid Arthritis Phase 4 Completed - -
NCT00552344 Crohn Disease Phase 3 Completed - -
更多
参考文献

[1] Bo Liu,et al. GPR55: from orphan to metabolic regulator? Pharmacol Ther. 2015 Jan;145:35-42.
[2] Fatemi I, et, al. The effect of intra-striatal administration of GPR55 agonist (LPI) and antagonist (ML193) on sensorimotor and motor functions in a Parkinson's disease rat model. Acta Neuropsychiatr. 2021 Feb;33(1):15-21.
[3] Hill JD, et, al. Activation of GPR55 increases neural stem cell proliferation and promotes early adult hippocampal neurogenesis. Br J Pharmacol. 2018 Aug;175(16):3407-3421.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.8954 mL
- 9.4770 mL
- 18.9540 mL
- 5 mM
- 0.3791 mL
- 1.8954 mL
- 3.7908 mL
- 10 mM
- 0.1895 mL
- 0.9477 mL
- 1.8954 mL

技术信息

CAS号	713121-80-3	储存条件	粉末 Sealed in dry,2-8°C 液体 -20°C:3-6 月 -80°C:12月
分子式	C28H25N5O4S	运输	蓝冰
分子量	527.59	别名	CID 1261822

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ML-193 Catalog No. CSN22976

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