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CID 2745687
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。
CID 2745687图片
CAS NO:264233-05-8
包装与价格：
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议

产品介绍
CID 2745687 是一种特异性、可逆和竞争性 GPR35 拮抗剂，Ki 为 12.8 nM。
Cas No.264233-05-8
化学名(E)-methyl 5-((2-(tert-butylcarbamothioyl)hydrazono)methyl)-1-(2,4-difluorophenyl)-1H-pyrazole-4-carboxylate
Canonical SMILESS=C(N/N=C/C1=C(C(OC)=O)C=NN1C(C(F)=C2)=CC=C2F)NC(C)(C)C
分子式C17H19F2N5O2S
分子量395.43
溶解度DMSO: 10 mg/ml
储存条件Store at -20°C
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

pIC50: 6.70 for human GPR35

CID-2745687 is a GPR35 antagonist. GPR35 is a poorly characterized member of the rhodopsinlike, class A subfamily of G protein-coupled receptors (GPCRs). GPCRs, based on the expression pattern, has been considered as a possible therapeutic target in conditions including diabetes, cardiovascular disease, as well as inflammation and pain.

In vitro: Previous study indicated that both CID-2745687 and ML-145 could competitively inhibit the effects of cromolyn disodium and zaprinast (two agonists sharing an overlapping binding site) on human GPR35. In contrast, though ML-145 antagonized the effects of pamoate competitively, CID-2745687 showed a noncompetitive fashion. Additionally, neither ML-145 nor CID-2745687 was able to antagonize the agonist effects at rodent ortholog of GPR35 [1].

In vivo: To test whether GPR35 contributes to the metabolic effect of Zaprinast, the retina from Cngb1/ mice was preincubated with a GPR35 antagonist, CID-2745687, followed by an additional Zaprinast treatment. Results showed that CID-2745687 did not block the effect of Zaprinast on glutamate and aspartate. Moreover, pamoic acid, the GPR35 agonist, did not change aspartate or glutamate levels [1].

Clinical trial: N/A

References:
[1] Jenkins L,Harries N,Lappin JE,MacKenzie AE,Neetoo-Isseljee Z,Southern C,McIver EG,Nicklin SA,Taylor DL,Milligan G. Antagonists of GPR35 display high species ortholog selectivity and varying modes of action. J Pharmacol Exp Ther.2012 Dec;343(3):683-95.
[2] Du J,Cleghorn WM,Contreras L,Lindsay K,Rountree AM,Chertov AO,Turner SJ,Sahaboglu A,Linton J,Sadilek M,Satrústegui J,Sweet IR,Paquet-Durand F,Hurley JB. Inhibition of mitochondrial pyruvate transport by zaprinast causes massive accumulation of aspartate at the expense of glutamate in the retina. J Biol Chem.2013 Dec 13;288(50):36129-40.