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.
Product Specifications
CAS Number
[1262238-11-8]
UNSPSC
12352005
Target
CCR
Type
Reference compound
Related Pathways
GPCR/G Protein; Immunology/Inflammation
Applications
COVID-19-immunoregulation
Field of Research
Inflammation/Immunology; Endocrinology
Assay Protocol
https://www.medchemexpress.com/INCB3344.html
Purity
99.08
Solubility
DMSO : 200 mg/mL (ultrasonic)
Smiles
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
Molecular Formula
C29H34F3N3O6
Molecular Weight
577.59
References & Citations
[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.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
CCR2
Available Sizes
Curated Selection
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