INCB-3284
INCB-3284 性质
| 沸点 | 703.7±60.0 °C(Predicted) |
|---|---|
| 密度 | 1.35±0.1 g/cm3(Predicted) |
| 储存条件 | Store at -20°C |
| 溶解度 | 可溶于DMSO（少许）、甲醇（少许） |
| 形态 | 固体 |
| 酸度系数(pKa) | 12.94±0.46(Predicted) |
| 颜色 | 黄色至深黄色 |
INCB-3284 用途与合成方法
|
MCP-1-hCCR2 3.7 nM (IC 50 ) |
INCB 3284 is a pentent, selective and orally bioavailable human CCR2 antagonist, inhibiting monocyte chemoattractant protein-1 binding to hCCR2, with an IC 50 of 3.7 nM. INCB 3284 also causes an IC 50 of 4.7 nM in antagonism of chemotaxis activity, an IC 50 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 IC 50 values of 6 and 2.6 nM, respectively.
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.
