Cis-INCB3344

Cis-INCB3344 is the isomer of INCB3344 (HY-50674), and can be used as an experimental control. 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

[1285539-85-6]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

CCR; Drug Isomer

Type

Reference compound

Related Pathways

GPCR/G Protein; Immunology/Inflammation; Others

Applications

Metabolism-protein/nucleotide metabolism

Field of Research

Endocrinology; Inflammation/Immunology

Assay Protocol

https://www.medchemexpress.com/cis-incb3344.html

Purity

95.10

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

O=C(NCC(N[C@H]1CN([C@@H]2CC[C@](C3=CC=C(OCO4)C4=C3)(O)CC2)C[C@@H]1OCC)=O)C5=CC=CC(C(F)(F)F)=C5

Molecular Formula

C29H34F3N3O6

Molecular Weight

577.59

Precautions

H302, H315, H319, H335

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]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.|[3]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.|[4]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.|[5]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.|[6]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.|[7]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.