| 产品描述: | 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 |
| 靶点: |
IC50: 221 nM (GPR55);CannabinoidReceptor |
| 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. |
| 参考文献: |
1. Heynen-Genel S, et, al. Screening for Selective Ligands for GPR55-Antagonists. Probe Reports from the NIH Molecular Libraries Program. 2010 Oct 30. 2. Kotsikorou E, et, al. Identification of the GPR55 antagonist binding site using a novel set of high-potency GPR55 selective ligands. Biochemistry. 2013 Dec 31;52(52):9456-69. 3. 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. 4. 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. |
| 溶解性: |
可溶于DMSO |
| 保存条件: |
2-8℃,避光 |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
1.895 ml |
9.477 ml |
18.954 ml |
| 5 mM |
0.379 ml |
1.895 ml |
3.791 ml |
| 10 mM |
0.19 ml |
0.948 ml |
1.895 ml |
| 50 mM |
0.038 ml |
0.19 ml |
0.379 ml |
|
| 注意: |
部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。 |