INCB3344_1262238-11-8_DataSheet_MedChemExpress

Product Name:

INCB3344CAS No.:

1262238-11-8Cat. No.:

HY-50674Product Data Sheet

MWt:

577.59Formula:

C29H34F3N3O6Purity :>98%

Solubility:

DMSO

Mechanisms:Biological Activity:

INCB3344is a novel,potent and selective small molecule antagonist of the mouse CCR2receptor;

Pathways:Immunology/Inflammation; Target:CCR Pathways:GPCR/G protein; Target:CCR INCB3344 is a novel, potent and selective small molecule antagonist of the mouse CCR2 receptor; inhibits the binding of CCL2 to mouse monocytes with nanomolar potency (IC50 = 10 nM).

IC50 value: 10 nM [1]

Target: CCR2In vitro: INCB3344 inhibits the binding of CCL2 to mouse monocytes with nanomolar potency (IC(50)= 10 nM) and displays dose-dependent inhibition of CCL2-mediated functional responses such as ERK phosphorylation and chemotaxis with similar potency. Against a panel of G protein-coupled receptors that includes other CC chemokine receptors, INCB3344 is at least 100-fold selective for CCR2 [1]. INCB3344 can also bind human CCR2 (hCCR2) with high affinity, having a dissociation References:

[1]. Brodmerkel CM, et al. Discovery and pharmacological characterization of a novel rodent-active

CCR2 antagonist, INCB3344. J Immunol. 2005 Oct 15;175(8):5370-8.[2].Shin N,et al.Pharmacological characterization of INCB3344,a small molecule antagonist of constant (K(d)) of approximately 5nM. The binding of the compound to the receptor is rapid and reversible. INCB3344 potently inhibits hCCR2 binding of monocyte chemoattractant protein-...[2]. Shin N, et al. Pharmacological characterization of INCB3344, a small molecule antagonist of

human CCR2. Biochem Biophys Res Commun. 2009 Sep 18;387(2):251-5.[3]. Chan CT, et al. Reversal of vascular macrophage accumulation and hypertension by a CCR2

antagonist in deoxycorticosterone/salt-treated mice. Hypertension. 2012 Nov;60(5):1207-12.Caution: Not fully tested. For research purposes only

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