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CCR2 antagonist 4 hydrochlorideCAS No. : 1313730-14-1
MCE 國際站:CCR2 antagonist 4 hydrochloride
產(chǎn)品活性:CCR2 antagonist 4 hydrochloride (Teijin compound 1 hydrochloride) 是一種高效、特異的 CCR2 拮抗劑,對 CCR2b 的 IC50 值為 180 nM。CCR2 antagonist 4 hydrochloride 對 MCP-1 誘導(dǎo)的趨化作用有較強(qiáng)的抑制作用,其 IC50 為 24 nM。
研究領(lǐng)域:GPCR/G Protein | Immunology/Inflammation
作用靶點(diǎn):CCR
In Vitro: Ile263 and Thr292 in CCR2 contribute significantly to binding of CCR2 antagonist 4 in CCR2. Residue Glu291 in TM7, a highly conserved residue in many CC chemokine receptors, contributes substantially to binding of the protonated CCR2 antagonist 4 hydrochloride, and CCL2. His121 on TM3 and Ile263 on TM6 also strongly interact with CCR2 antagonist 4 hydrochloride.
In Vivo: In ApoE-deficient mice, Vp-TSL targets specifically aortic plaque endothelial VCAM-1 and CCR2 antagonist 4 hydrochloride reduces the mouse monocyte/macrophage cell line (RAW 264.7) adhesion/ infiltration into the aorta.
相關(guān)產(chǎn)品:Bioactive Compound Library Plus | GPCR/G Protein Compound Library | Immunology/Inflammation Compound Library | Small Molecule Immuno-Oncology Compound Library | Pirfenidone | Maraviroc | RS 504393 | INCB3344 | PF-4136309 | BX471 | Bindarit | TAK-779 | RS102895 hydrochloride | AZ084 | CCR6 inhibitor 1 | TAK-220 | 7,4'-Dihydroxyflavone | CCR2-RA-[R] | INCB 3284 | J-113863 | Vicriviroc maleate | DAPTA | K777 | SB297006 | LMD-009 | ZK756326 dihydrochloride | CCR2 antagonist 3 | CCR2 antagonist 4 | Aplaviroc | AZD2423 | CCR2 antagonist 1
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