INCB 3284 dimesylate

Cat. No. 4306

INCB 3284 dimesylate C26H31F3N4O4.2CH4O3S [887401-93-6]

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Chemical Name: N-[2-[[(3R)-1-[trans-4-Hydroxy-4-(6-methoxy-3-pyridinyl)cyclohexyl]-3-pyrrolidinyl]amino]-2-oxoethyl]-3-(trifluoromethyl)-benzamide dimethanesulfonate

Biological Activity

Potent, selective hCCR2 antagonist. Exhibits potent antagonism against monocyte chemoattractant molecule binding to hCCR2 and chemotaxis activity (IC50 values are 3.7 and 4.7 nM respectively). Also displays weak hERG activity; inhibits the hERG potassium current (IC50 = 84μM). Orally bioavailable.

Technical Data

M.Wt:
712.76
Formula:
C26H31F3N4O4.2CH4O3S
Solubility:
Soluble to 100 mM in water and to 100 mM in DMSO
Purity:
>98 %
Storage:
Store at -20°C
CAS No:
887401-93-6

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Product Datasheet / Safety Data Sheet

Xue et al (2011) Discovery of INCB3284, a potent, selective, and orally bioavailable hCCR2 antagonist. ACS.Med.Chem.Lett. 2 450.

If you know of a relevant reference for this product please let us know.

Citations are publications that use Tocris products. Selected citations for INCB 3284 dimesylate include:

Liu et al (2016) Cancer-associated fibroblasts promote hepatocellular carcinoma metastasis through chemokine-activated hedgehog and TGF-β pathways. Cancer Lett. 379 49. PMID: 27216982.

Zhou et al (2015) Klotho gene deficiency causes salt-sensitive hypertension via monocyte chemotactic protein-1/CC chemokine receptor 2-mediated inflammation. Nat Commun 26 121. PMID: 24904083.

McMillin et al (2014) Neuronal CCL2 is upregulated during hepatic encephalopathy and contributes to microglia activation and neurological decline. J Neuroinflammation 11 121. PMID: 25012628.

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Keywords: INCB 3284 dimesylate, supplier, INCB3284, CCR2, antagonist, antagonists, hCCR2, human, chemokine, receptor, receptors, Tocris Bioscience, Chemokine CC Receptor Antagonist products

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