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INCB 3284 dimesylate

CAS No. : 887401-93-6

MCE 站：INCB 3284 dimesylate

产品活性：INCB 3284 dimesylate 是一种有效的，选择性的人 CCR2 拮抗剂，能够抑制单核细胞趋化蛋白 1 与 hCCR2 结合，IC₅₀ 值为 3.7 nM。INCB 3284 dimesylate 可用于急性肝功能衰竭的研究。

研究领域：GPCR/G Protein  |  Immunology/Inflammation

作用靶点：CCR

In Vitro: 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 (1 mg/kg/day, ip) reduces liver damage, and decreases microglia activation in AOM-treated mice via inhibition on CCR2. 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.

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