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INCB3344CCR2 chemokine receptor antagonist

INCB3344

Catalog No. A3494
Size Price Stock Qty
5mg $256.00 In stock
10mg $336.00 In stock
50mg $906.00 In stock
100mg $1,402.00 In stock

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

INCB3344

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Chemical Properties

Cas No. 1262238-11-8 SDF Download SDF
Synonyms INCB 3344; INCB-3344
Chemical Name N-[2-[[(3S,4S)-1-[4-(1,3-benzodioxol-5-yl)-4-hydroxycyclohexyl]-4-ethoxypyrrolidin-3-yl]amino]-2-oxoethyl]-3-(trifluoromethyl)benzamide
Canonical SMILES CCOC1CN(CC1NC(=O)CNC(=O)C2=CC(=CC=C2)C(F)(F)F)C3CCC(CC3)(C4=CC5=C(C=C4)OCO5)O
Formula C29H34F3N3O6 M.Wt 577.24
Solubility Soluble in DMSO Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

Background

INCB3344 is a novel potent and selective antagonist of CCR2 receptor, which possesses an IC 50 of 10 nM for CCL2. [1]

CCR2 is a chemokine receptor mainly expressed on monocytes which acts as the key receptor in mediating their tissue influx in the context of immune-based inflammation. CCR2 is a G protein-coupled receptor (GPCR), whose ligands include the chemokines MCP family, including CCL2, CCL7, CCL8. These ligands bind CCR2 receptor with high affinity and elicit a chemotactic signal which leads to directed migration of the receptor-bearing cells. CCL2 has been shown to be relevant in high concentrations in various inflammatory lesions, implicating this chemokine as a physiologically important chemotactic signal for monocytes. [1]

Characterization of the pharmacological activity of INCB3344 was first evaluated by testing its ability to inhibit CCL2 binding to CCR2 in a whole cell binding assay using a murine monocyte cell line, WEHI-274.1 and 125I-labeled mCCL2 as a tracer. The binding IC 50 of INCB3344 in this assay was determined to be 10±5 nM, and inhibition greater than 90% binding was observed at a concentration of 90nM . The chemotaxis inhibitory activity of different concentrations of INCB3344 was evaluated using 30nM mCCL2 as the agonist. The result showed a similar potency to the binding assay. Selectivity of INCB3344 was evaluated against a panel of GPCRs including several human chemokine receptors using radioligand binding assays. Results from these studies demonstrate at least 100-fold selectivity of INCB3344 against all of the receptors tested. [1]

INCB3344 treatment results in a dose-dependent inhibition of macrophage influx in a mouse delayed-type hypersensitivity model. The histopathological analysis of tissues from the delayed-type hypersensitivity model illustrates that inhibitory activity of CCR2 leads to a substantial reduction in tissue inflammation. [1]

Reference:
[1].  Brodmerkel C M, Huber R, Covington M, et al. Discovery and pharmacological characterization of a novel rodent-active CCR2 antagonist, INCB3344[J]. The Journal of Immunology, 2005, 175(8): 5370-5378.