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INCB 3284

Catalog No. T11648 CAS 887401-92-5

INCB 3284, a potent and selective human CCR2 antagonist with an oral bioavailability, is utilized in the study of acute liver failure. It effectively inhibits the binding of monocyte chemoattractant protein-1 (MCP-1) to hCCR2, demonstrating an IC50 of 3.7 nM.

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INCB 3284, CAS 887401-92-5

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2 mg	5 days	$ 39.00

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Storage & Solubility Information

Description	INCB 3284, a potent and selective human CCR2 antagonist with an oral bioavailability, is utilized in the study of acute liver failure. It effectively inhibits the binding of monocyte chemoattractant protein-1 (MCP-1) to hCCR2, demonstrating an IC50 of 3.7 nM.
Targets&IC50	MCP-1-hCCR2:3.7 nM
In vitro	INCB 3284 is a potent, selective, and orally bioavailable human CCR2 antagonist that exhibits high efficacy in inhibiting monocyte chemoattractant protein-1 binding to its receptor with an IC50 of 3.7 nM. It also demonstrates significant antagonistic activity against chemotaxis with an IC50 of 4.7 nM and effectively inhibits CCR2-mediated signaling events, including intracellular calcium mobilization and ERK phosphorylation, with IC50 values of 6 nM and 2.6 nM, respectively. Additionally, INCB 3284 inhibits the hERG potassium current with an IC50 of 84 μM. However, it shows no effect on CCR1, CCR3, CCR5, CXCR3, CXCR5, or other GPCRs at a concentration of 1 μM.
In vivo	INCB 3284 markedly lowers the ratio of phosphorylated ERK1/2 (pERK1/2) to total ERK1/2 (tERK1/2), diminishes G-protein signaling pathway activity, and suppresses the production of proinflammatory cytokines in cortex lysates from mice treated with azoxymethane (AOM). Additionally, when administered at a dose of 1 mg/kg/day intraperitoneally (ip), INCB 3284 mitigates liver damage and attenuates microglia activation in AOM-treated mice through the inhibition of CCR2.

Molecular Weight	520.553
Formula	C26H31F3N4O4
CAS No.	887401-92-5

Storage

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

Solubility Information

DMSO: 83.3 mg/mL (160.03 mM)

References 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 887401-92-5 Others INCB3284 INCB-3284 inhibitor inhibit

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