CCR2-RA-[R] - 10mM in DMSO , CAS No.512177-83-2

CAS: 512177-83-2 Cat. No.: C656241 Fórmula: C₁₈H₁₉ClFNO₃ Peso molecular: 351.8 PubChem CID: 12093170

GRADE & PURITY 10mM in DMSO

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Descripción general

CCR2-RA-[R] is an allosteric antagonist of the C-C chemokine receptor type 2 (CCR2) with an IC 50 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 [ 125 I]CCL2 from CCR2 with an pIC 50 value of 6.1. The pK D 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”. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

IC50& Target:CCR2 103 nM (IC 50 , in U2OS-CCR2 cells)

Specifications

Especificaciones y pureza

10mM in DMSO

Mecanismos bioquímicos y fisiológicos

CCR2-RA-[R] is an allosteric antagonist of the C-C chemokine receptor type 2 (CCR2) with an IC 50 of 103 nM.

Condiciones de almacenamiento de almacenamiento

Store at -80°C

Enviado en

Dry ice packs + Cold packs

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Tipo de acción

ANTAGONIST

Nombres e identificadores

Isómeros SMILES

CC(=O)C1=C(C(=O)N([C@@H]1C2CCCCC2)C3=C(C=C(C=C3)Cl)F)O

PubChem CID

12093170

Peso molecular

351.8

Objetivos asociados (humanos)

CCR2 Tchem C-C chemokine receptor type 2 (0 Activities)

Discover Target: CCR2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)