INCB3344

INCB3344 is a potent, selective and orally bioavailable CCR2 antagonist with IC50 values of 5.1 nM (hCCR2) and 9.5 nM (mCCR2) in binding antagonism and 3.8 nM (hCCR2) and 7.8 nM (mCCR2) in antagonism of chemotaxis activity.

1262238-11-8

12352005

CCR

Reference compound

GPCR/G Protein; Immunology/Inflammation

COVID-19-immunoregulation

Inflammation/Immunology; Endocrinology

https://www.medchemexpress.com/INCB3344.html

99.08

DMSO : 200 mg/mL (ultrasonic)

CCO[C@H]1CN([C@]2([H])CC[C@@](CC2)(C3=CC4=C(OCO4)C=C3)O)C[C@@H]1NC(CNC(C5=CC(C(F)(F)F)=CC=C5)=O)=O

C29H34F3N3O6

577.59

[1]Xue CB, et al. Discovery of INCB3344, a potent, selective and orally bioavailable antagonist of human and murine CCR2. Bioorg Med Chem Lett. 2010 Dec 15;20 (24) :7473-8|[2]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.|[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.|[4]Dansereau MA, et al. Spinal CCL2 pronociceptive action is no longer effective in CCR2 receptor antagonist-treated rats. J Neurochem. 2008 Jul;106 (2) :757-69.|[5]Zhao W, et al. Enrichment of Ly6Chi monocytes by multiple GM-CSF injections with HBV vaccine contributes to viral clearance in a HBV mouse model. Hum Vaccin Immunother. 2017 Dec 2;13 (12) :2872-2882.|[6]Aye-Mon A, et al. CCR2 upregulation in DRG neurons plays a crucial role in gastric hyperalgesia associated with diabetic gastropathy. Mol Pain. 2018 Jan-Dec;14:1744806917751322.|[7]Cassini MF, et al. Mcp1 Promotes Macrophage-Dependent Cyst Expansion in Autosomal Dominant Polycystic Kidney Disease. J Am Soc Nephrol. 2018 Oct;29 (10) :2471-2481.

Room Temperature

-20°C, 3 years; 4°C, 2 years (Powder)

Reference compound1

No Development Reported