ML-193
| 规格 | 价格 | 货期 | 数量 |
|---|---|---|---|
| 5mg | 请咨询 | 10-15工作日发货 | |
| 10mg | 请咨询 | 10-15工作日发货 | |
| 25mg | 请咨询 | 10-15工作日发货 |
特色产品
- 用于免疫印迹和质谱分析等后续操作
- 适用于30 KDa-130 KDa大小的蛋白
- 可将信号灵敏度提高100倍
- 同时保持稳定的特异性和分辨率
- 提供更高的转录效率并抑制免疫激活
- 使用5-moUTP和Cy5-utp修饰
产品描述
IC50: 221 nM
ML-193 is a GPR55 antagonist.
GPR55 is a class A G protein-coupled receptor (GPCR) that has been implicated in inflammatory pain, neuropathic pain, metabolic disorder, bone development, and cancer. Initially deorphanized as a cannabinoid receptor, GPR55 has been shown to be activated by non-cannabinoid ligands such as l-α-lysophosphatidylinositol (LPI).
In vitro: Previous study found that for antagonist activity in the β-arrestin trafficking assay, ML193 and its two close analogs (ML191 and ML192) could inhibit trafficking induced by 10 μM LPI with IC50 values of 0.22 ± 0.03, 1.08 ± 0.03 and 0.70 ± 0.05μM, respectively.In addition, it was also found that ML193, ML191 and ML192 was able to inhibit trafficking induced by 1 μM ML186 with IC50 values of 0.12 ±0.02, 1.03 ± 0.03 and 0.29 ± 0.09 μM, respectively [1].
In vivo: Animal study showd that ML-193 was able to block the increases in intracellular calcium levels that was induced by lysophosphatidylinositol (LPI) in dissociated rat periaqueductal gray neurons and could also modulate pain perception in LPI-treated rats, suggesting that interfering with GPR55 signaling in the PAG might promote analgesia [2].
Clinical trial: So far, no clinical study has been conducted.
References:
[1] Kotsikorou, E. ,Sharir, H.,Shore, D.M., et al. Identification of the GPR55 antagonist binding site using a novel set of high-potency GPR55 selective ligands. Biochemistry 52(52), 9456-9469 (2013).
[2] Deliu, E. ,Sperow, M.,Console-Bram, L., et al. The lysophosphatidylinositol receptor GPR55 modulates pain perception in the periaqueductal gray. Mol.Pharmacol. 88(2), 265-272 (2015).
产品性质
| 物理外观 | A crystalline solid |
| CAS号 | 713121-80-3 |
| 分子式 | C28H25N5O4S |
| 分子量 | 527.6 |
| 化学名称 | N-[4-[[(3,4-dimethyl-5-isoxazolyl)amino]sulfonyl]phenyl]-6,8-dimethyl-2-(2-pyridinyl)-4-quinolinecarboxamide |
| 溶解度 | ≤0.1mg/ml in ethanol;2mg/ml in DMSO;3mg/ml in dimethyl formamide |
| SMILES | O=C(C1=C(C=C(C)C=C2C)C2=NC(C3=CC=CC=N3)=C1)NC4=CC=C(S(NC5=C(C)C(C)=NO5)(=O)=O)C=C4 |
| 存储条件 | -20°C |
| 运输条件 | 蓝冰 |
产品应用 (实验数据来自文献,APExBIO并未验证,仅供参考)
IC50和靶点
| 生物活性描述 | ML-193(CID 1261822)是一种强效的 GPR55 选择性拮抗剂,IC50 为 221 nM。ML-193 对 GPR55 的选择性超过 GPR35、CB1 和 CB2 的 27 倍。ML-193 可以改善帕金森病(PD)大鼠的运动和感觉运动障碍。 |



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