CCR2-RA-[R]( CCR2-RA [R] )

Catalog No. M14769 CAS No. 512177-83-2

COA

Datasheet

HNMR

HPLC

MSDS

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Product Name

CCR2-RA-[R]
Note

Research use only, not for human use.
Brief Description

A potent, selective, allosteric CCR2 antagonist with IC50 of 103 nM.
Description

A potent, selective, allosteric CCR2 antagonist with IC50 of 103 nM.
In Vitro

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. 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. CCR2-RA-[R] inhibits CCR2 non-competitively by blocking activation-associated conformational changes and formation of the G protein-binding interface. 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”.
In Vivo

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Synonyms

CCR2-RA [R]
Pathway

GPCR/G Protein
Target

Chemokine Receptor
Recptor

Chemokine Receptor
Research Area

——
Indication

——

CAS Number

512177-83-2
Formula Weight

351.802
Molecular Formula

C18H19ClFNO3
Purity

>98% (HPLC)
Solubility

DMSO : ≥ 125 mg/mL 355.32 mM; H2O : < 0.1 mg/mL
SMILES

O=C1N(C2=CC=C(Cl)C=C2F)[C@H](C3CCCCC3)C(C(C)=O)=C1O
Chemical Name

(R)-4-acetyl-1-(4-chloro-2-fluorophenyl)-5-cyclohexyl-3-hydroxy-1,5-dihydro-2H-pyrrol-2-one

1. Zheng Y, et al. Nature. 2016 Dec 15;540(7633):458-461. 2. Zweemer AJ, et al. Mol Pharmacol. 2013 Oct;84(4):551-61.

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