ccr4 antagonist 2

CCR4 antagonist 2 (Compound 31) is a novel, potent, orally bioavailable small molecule antagonist of CC chemokine receptor 4 (CCR4) that inhibits Treg trafficking into the Tumor Microenvironment without suppressing the number of Treg in healthy tissues. CCR4 antagonist 2 (Compound 31) exhibits IC50 values of Ca2+ flux and [chemotaxis] CTX at 40 nM and 70 nM, respectively.

C 021 dihydrochloride is a potent CCR4 antagonist. C-021 (4-Quinazolinamine, 2-[1,4'-bipiperidin]-1'-yl-N-cycloheptyl-6,7-dimethoxy-) dihydrochloride potently inhibits functional chemotaxis in humans and mice with IC50s of 140 nM and 39 nM, respectively. It effectively prevents human CCL22-derived [35S]GTPγS from binding to the receptor (IC50: 18 nM).

AZD-1678, [3-(2-(2-(2-hydroxyethoxy)ethoxy)ethoxy)-2-methoxyphenyl]-(2-(4-((E)-2-(2-(thiophen-3-yl)vinyl)pyrrolidin-1-yl)methyl)benzyl)amine, is a potent CCR4 receptor antagonist.

GSK2239633 is a potent CC-chemokine receptor 4 antagonist with pIC50 of 7.9. The CC-chemokine receptor 4 (CCR4) is thought potentially to play a critical role in asthma pathogenesis due to its ability to recruit type 2 T-helper lymphocytes to the inflamed airways. Therefore, CCR4 provides an excellent target for anti-inflammatory therapy.