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INCB 3284 dimesylate

Catalog No. T11647   CAS 887401-93-6

INCB 3284 dimesylate is a selective and orally bioavailable human CCR2 antagonist, inhibiting monocyte chemoattractant protein-1 binding to hCCR2 (IC50: 3.7 nM). It can be used in the research of acute liver failure.

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INCB 3284 dimesylate Chemical Structure
INCB 3284 dimesylate, CAS 887401-93-6
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Biological Description
Chemical Properties
Storage & Solubility Information
Description INCB 3284 dimesylate is a selective and orally bioavailable human CCR2 antagonist, inhibiting monocyte chemoattractant protein-1 binding to hCCR2 (IC50: 3.7 nM). It can be used in the research of acute liver failure.
Targets&IC50 MCP-1-hCCR2:3.7 nM
In vitro INCB 3284 causes an IC50 of 4.7 nM in antagonism of chemotaxis activity, an IC50 of 84 μM in inhibition of the hERG potassium current. However, INCB 3284 has no effec on CCR1, CCR3, CCR5, CXCR3, and CXCR5, or additional GPCRs at a concentration of 1 μM. Moreover, INCB 3284 potently inhibits CCR2-mediated signaling events such as intracellular calcium mobilization and ERK phosphorylation with IC50 values of 6 and 2.6 nM, respectively.INCB 3284 dimesylate is a pentent, selective and orally bioavailable human CCR2 antagonist, inhibiting monocyte chemoattractant protein-1 binding to hCCR2, with an IC50 of 3.7 nM.?INCB 3284 also causes an IC50 of 4.7 nM in antagonism of chemotaxis activity, an IC50 of 84 μM in inhibition of the hERG potassium current.?However, INCB 3284 has no effec on CCR1, CCR3, CCR5, CXCR3, and CXCR5, or additional GPCRs at a concentration of 1 μM.?Moreover, INCB 3284 potently inhibits CCR2-mediated signaling events such as intracellular calcium mobilization and ERK phosphorylation with IC50 values of 6 and 2.6 nM, respectively.
In vivo INCB 3284 also significantly reduces the pERK1/2 to tERK1/2 ratio, as well as G-protein signaling pathway activity and proinflammatory cytokine production in cortex lysates from mice administed with azoxymethane.INCB 3284 (1 mg/kg/day, ip) reduces liver damage, and decreases microglia activation in AOM-treated mice via inhibition on CCR2.
Molecular Weight 712.76
Formula C28H39F3N4O10S2
CAS No. 887401-93-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 83.3 mg/mL (116.87 mM)

TargetMolReferences and Literature

1. Xue CB, et al. Discovery of INCB3284, a Potent, Selective, and Orally Bioavailable hCCR2 Antagonist. ACS Med Chem Lett. 2011 Mar 31;2(6):450-4. 2. McMillin M, et al. Neuronal CCL2 is upregulated during hepatic encephalopathy and contributes to microglia activation and neurological decline. J Neuroinflammation. 2014 Jul 10;11:121.

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Keywords

INCB 3284 dimesylate 887401-93-6 Others INCB-3284 Dimesylate INCB 3284 Dimesylate INCB3284 INCB3284 Dimesylate INCB-3284 INCB 3284 inhibitor inhibit

 

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