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cis-INCB3344
$120 – $980
Products Details
Product Description
– cis-INCB3344 is the inactive 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.
Web ID
– HY-77111
Storage Temperature
– -20°C, 3 years; 4°C, 2 years (Powder)
Shipping
– Room Temperature
Molecular Formula
– C29H34F3N3O6
References
– [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.
CAS Number
– 1285539-85-6
Molecular Weight
– 577.59
Compound Purity
– 98.75
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
Clinical Information
– No Development Reported
Research Area
– Endocrinology; Inflammation/Immunology
Solubility
– 10 mM in DMSO
Target
– Others
Pathway
– Others
Product type
– Reference compound
Disclaimer: All products are for research use only unless clearly stated otherwise on the product datasheet. Datasheets provided on the website are drafts for reference purpose only and you are requested to always refer to the hard copy included in the kit for your experimentation.
