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CCR2-RA-[R]
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。
CCR2-RA-[R]图片
CAS NO:512177-83-2
包装与价格:
包装价格(元)
2 mg电议
5 mg电议
10 mg电议
25 mg电议
50 mg电议
100 mg电议
200 mg电议
1 mL*10 mM(in DMSO)电议

产品名称
(5R)-4-乙酰基-1-(4-氯-2-氟苯基)-5-环己基-1,5-二氢-3-羟基-2H-吡咯-2-酮
产品介绍
CCR2-RA-[R] 是一种 C-C 趋化因子受体 2 型 (CCR2) 变构拮抗剂,IC50值为103 nM。

产品描述

CCR2-RA-[R] is a C-C chemokine receptor type 2 (CCR2) allosteric antagonist (IC50: 103 nM).

体外活性

CCR2-RA-[R] inhibits CCR2 non-competitively by blocking activation-associated conformational changes and formation of the G protein-binding interface. CCR2-RA-[R] displaces [125I]CCL2 from CCR2 with an pIC50 value of 6.1. The pKD of CCR2-RA-[R] for CCR2 and CCR5 is 8.8±0.1 and 7.0±0.1, respectively[2]. The chemokine receptor CCR2 is a G protein-coupled receptor that is involved in many diseases characterized by chronic inflammation, and therefore a large variety of CCR2 small molecule antagonists has been developed. The binding pocket of CCR2-RA-[R] is highly enclosed and possesses a balanced combination of hydrophobic and polar features, all of which favors pocket “druggability”[3].

Cas No.

512177-83-2

分子式

C18H19ClFNO3

分子量

351.8

别名

(5R)-4-乙酰基-1-(4-氯-2-氟苯基)-5-环己基-1,5-二氢-3-羟基-2H-吡咯-2-酮

储存和溶解度

DMSO:125 mg/mL (355.32 mM)
H2O:< 0.1 mg/mL (insoluble)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years