您好，欢迎来到试剂信息网！ [登录] [免费注册]
试剂信息网
发布求购
位置：首页 > 产品库 > ML-193
立即咨询
咨询类型：
     
*姓名：
*电话：
*单位：
Email：
*留言内容：
请详细说明您的需求。
*验证码：
 
ML-193
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
ML-193图片
CAS NO:713121-80-3
包装与价格：
包装价格(元)
1mg电议
5mg电议
10mg电议
25mg电议

产品介绍
ML-193 (CID 1261822) 是一种有效的选择性 GPR55 拮抗剂，IC50 为 221 nM。
Cas No.713121-80-3
别名CID-1261822
化学名N-[4-[[(3,4-dimethyl-5-isoxazolyl)amino]sulfonyl]phenyl]-6,8-dimethyl-2-(2-pyridinyl)-4-quinolinecarboxamide
Canonical SMILESO=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
分子式C28H25N5O4S
分子量527.6
溶解度≤0.1mg/ml in ethanol;2mg/ml in DMSO;3mg/ml in dimethyl formamide
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
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).