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首页 / 抑制剂/激动剂 / G蛋白偶联受体/G蛋白 / GPCR / ML-193

ML-193 {[allProObj[0].p_purity_real_show]}

货号：A811582 同义名： CID 1261822

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

ML-193 化学结构 CAS号：713121-80-3
ML-193 化学结构
CAS号：713121-80-3
ML-193 3D分子结构
CAS号：713121-80-3
ML-193 化学结构 CAS号：713121-80-3
ML-193 3D分子结构 CAS号：713121-80-3
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ML-193 纯度/质量文件 产品仅供科研

货号：A811582 标准纯度： {[allProObj[0].p_purity_real_show]}
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ML-193 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].

ML-193 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 - -

ML-193 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.

ML-193 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.90mL

0.38mL

0.19mL

9.48mL

1.90mL

0.95mL

18.95mL

3.79mL

1.90mL

ML-193 技术信息

CAS号713121-80-3
分子式C28H25N5O4S
分子量 527.59
SMILES Code O=C(C1=CC(C2=NC=CC=C2)=NC3=C(C)C=C(C)C=C13)NC4=CC=C(S(=O)(NC5=C(C)C(C)=NO5)=O)C=C4
MDL No. MFCD05999971
别名 CID 1261822
运输蓝冰
InChI Key HTSLEZOTMYUPLU-UHFFFAOYSA-N
Pubchem ID 1261822
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Sealed in dry, 2-8°C

Tags: ML-193 | 713121-80-3 | CID 1261822 | ML193 | ML 193 | CID1261822 | CID-1261822 | GPR55 Antagonist | GPCR/G Protein | Neuronal Signaling | GPR55 | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | ML-193 纯度/质量文件 | ML-193 生物活性 | ML-193 临床数据 | ML-193 参考文献 | ML-193 实验方案 | ML-193 技术信息

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