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Teijin compound 1
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
Teijin compound 1图片
CAS NO:1313730-14-1
包装与价格：
包装价格(元)
10mg电议
50mg电议

产品介绍
Teijin Compound 1 (Teijin Compound 1 hydrochloride) 是一种有效的特异性 CCR2 拮抗剂，对 CCR2b 的 IC50 值为 180 nM。
Cas No.1313730-14-1
别名Teijin compound 1 hydrochloride
化学名(S)-N-(2-((1-(4-chlorobenzyl)pyrrolidin-3-yl)amino)-2-oxoethyl)-3-(trifluoromethyl)benzamide hydrochloride
Canonical SMILESClC1=CC=C(C=C1)CN2C[C@H](CC2)NC(CNC(C3=CC=CC(C(F)(F)F)=C3)=O)=O.Cl
分子式C21H21ClF3N3O2.HCl
分子量476.32
溶解度DMSO: 100 mM,Water: 10 mM
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Teijin compound 1 is a specific CCR 2 antagonist with IC50s of 24 and 180 nM in chemotaxis and binding assay, respectively.

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 Teijin compound 1, and CCL2. His121 on TM3 and Ile263 on TM6 also strongly interact with Teijin compound 1[2].

In ApoE-deficient mice, Vp-TSL targets specifically aortic plaque endothelial VCAM-1 and Teijin compound 1 reduces the mouse monocyte/macrophage cell line (RAW 264.7) adhesion/ infiltration into the aorta[3].

References:
[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.