INCB 3284

An antagonist of the MCP-1 receptor CCR2

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Background

CCR2 is the receptor for the chemokine CCL2, known commonly as monocyte chemotactic protein-1 (MCP-1). INCB 3284 is a potent, selective, and orally bioavailable antagonist of monocyte chemotactic protein-1 binding to CCR2 (IC₅₀ = 3.7 nM).¹ For comparison, it has no significant inhibitor action at over 50 ion channels, transporters, GPCRs, and other chemokine receptors when tested at a concentration of 1 μM.¹ INCB 3284 inhibits chemotaxis in vitro (IC₅₀ = 4.7 nM) and displays acceptable oral bioavailability in mice, rats, dogs, monkeys, and chimpanzees.¹

1.Xue, C.B., Feng, H., Cao, G., et al.Discovery of INCB3284, a potent, selective, and orally bioavailable hCCR2 antagonistACS Med. Chem. Lett.2450-454(2011)

Protocol

Animal experiment:

Mice[2]Male C57Bl/6 mice (20 to 25 g) are given free access to water and rodent chow and are housed in constant temperature, humidity, and 12 h light-dark cycling. Acute liver failure is induced via a single intraperitoneal (ip) injection of 100 mg/kg of azoxymethane (AOM). In parallel, systemic inhibition of CCR2 and CCR4 activity is accomplished via pretreatment with INCB 3284 (1 mg/kg/day ip) or C021 (1 mg/kg/day ip) for 3 days prior to injection of AOM. Following injection, mice are placed on heating pads adjusted to 37°C and monitored frequently for signs of neurological decline. To reduce the impacts of hypoglycemia and dehydration, cage floors are supplied with hydrogel and rodent chow and after 12 h, and every subsequent 4 h, mice are injected subcutaneously with 5% dextrose in 250 μL of saline. If mice undergo a 20% or greater weight loss they are removed from the study[2].

参考文献:

[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.