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首页-小分子抑制剂&激动剂-GPCR-Chemokine Receptor (CCR and CXCR)-CCR4-IN-22
CCR4-IN-22

Chemical Structure : CCR4-IN-22

CAS No.: 668980-17-4

CCR4-IN-22 (Compound 22, CCR4 antagonist 4)

货号: PC-73263Not For Human Use, Lab Use Only.

CCR4-IN-22 (Compound 22) is a potent, selective CCR4 antagonist with IC50 of 20 nM, efficiently inhibits CCR4-mediated Ca2+ mobilization and chemotaxis in vitro with IC50 of 3 and 7 nM, repectively.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

CCR4-IN-22 (Compound 22) is a potent, selective CCR4 antagonist with IC50 of 20 nM, efficiently inhibits CCR4-mediated Ca2+ mobilization and chemotaxis in vitro with IC50 of 3 and 7 nM, repectively.
Compound 22 displays >500-fold less effective against other chemokine receptors (CCR2, CCR3 and CXCR3). and GPCRs (5-HT1A, 5-HT6 and 5-HT7).
Compound 22 suppressed eosinophil accumulation in the lungs of antigenimmunized mice in vivo, efficacious in a murine allergic inflammation model (ED50 10 mg/kg).
Compound 22, as well as anti-CCL17 or anti-CCL22 antibody selectively suppressed accumulation of Th2 cells and eosinophils in the lungs of Th2-transferred and OVA-challenged mice.
Compound 22 also inhibited bronchial hyperresponsiveness but had little effect on goblet cell hyperplasia in Th2-transferred and OVA-challenged mice.

物理化学性质&存储条件

分子量 500.428
分子式 C24H27Cl2N7O
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(R)-(4-(4-((2,4-dichlorobenzyl)amino)pyrido[2,3-d]pyrimidin-2-yl)piperazin-1-yl)(piperidin-2-yl)methanone

参考文献

1. Ashok V Purandare, et al. Bioorg Med Chem Lett. 2007 Feb 1;17(3):679-82.

2. O Kaminuma, et al. Clin Exp Allergy. 2012 Feb;42(2):315-25.

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