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CCR2 antagonist 4 Sale

(Synonyms: Teijin compound 1) 目录号 : GC60679

CCR2antagonist4(Teijincompound1)是一种高效、特异的CCR2拮抗剂,对CCR2b的IC50值为180nM。CCR2antagonist4对MCP-1诱导的趋化作用有较强的抑制作用,其IC50为24nM。

CCR2 antagonist 4 Chemical Structure

Cas No.:226226-39-7

规格 价格 库存 购买数量
5mg
¥1,710.00
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Sample solution is provided at 25 µL, 10mM.

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产品描述

CCR2 antagonist 4 (Teijin compound 1) is a potent and specific CCR2 antagonist, with IC50s of 180 nM for CCR2b. CCR2 antagonist 4 potently inhibits MCP-1-induced chemotaxis with an IC50 of 24 nM[1].

Ile263 and Thr292 in CCR2 contribute significantly to binding of Teijin compound 1 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, and CCL2. His121 on TM3 and Ile263 on TM6 also strongly interact with CCR2 antagonist 4[2].In ApoE-deficient mice, Vp-TSL targets specifically aortic plaque endothelial VCAM-1 and CCR2 antagonist 4 reduces the mouse monocyte/macrophage cell line (RAW 264.7) adhesion/ infiltration into the aorta[3].

[1]. Moree WJ, et al. Potent antagonists of the CCR2b receptor. Part 3: SAR of the (R)-3-aminopyrrolidine series. Bioorg Med Chem Lett. 2008 Mar 15;18(6):1869-73. [2]. Hall SE, et al. Elucidation of binding sites of dual antagonists in the human chemokine receptors CCR2 and CCR5. Mol Pharmacol. 2009 Jun;75(6):1325-36. [3]. Calin M, et al. VCAM-1 directed target-sensitive liposomes carrying CCR2 antagonists bind to activated endothelium and reduce adhesion and transmigration of monocytes. Eur J Pharm Biopharm. 2015 Jan;89:18-29.

Chemical Properties

Cas No. 226226-39-7 SDF
别名 Teijin compound 1
Canonical SMILES O=C(NCC(N[C@H]1CN(CC2=CC=C(Cl)C=C2)CC1)=O)C3=CC=CC(C(F)(F)F)=C3
分子式 C21H21ClF3N3O2 分子量 439.86
溶解度 DMSO: ≥ 50 mg/mL (113.67 mM) 储存条件 Store at -20°C
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1 mM 2.2735 mL 11.3673 mL 22.7345 mL
5 mM 0.4547 mL 2.2735 mL 4.5469 mL
10 mM 0.2273 mL 1.1367 mL 2.2735 mL
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