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CID 2745687

Catalog No.
B7635
GPR35 antagonist
Grouped product items
SizePriceStock Qty
5mg
$104.00
Ship with 5-10 days
10mg
$158.00
Ship with 5-10 days
25mg
$365.00
Ship with 5-10 days
50mg
$677.00
Ship with 5-10 days

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

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.

Chemical Properties

Physical AppearanceA crystalline solid
StorageStore at -20°C
M.Wt395.43
Cas No.264233-05-8
FormulaC17H19F2N5O2S
SolubilitySoluble in DMSO
Chemical Name(E)-methyl 5-((2-(tert-butylcarbamothioyl)hydrazono)methyl)-1-(2,4-difluorophenyl)-1H-pyrazole-4-carboxylate
SDFDownload SDF
Canonical SMILESS=C(N/N=C/C1=C(C(OC)=O)C=NN1C(C(F)=C2)=CC=C2F)NC(C)(C)C
Shipping ConditionEvaluation sample solution: ship with blue ice. All other available sizes: ship with RT, or blue ice upon request.
General tipsFor obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months.

Quality Control

Quality Control & MSDS

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Chemical structure

CID 2745687