INCB-3284
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- CAS号:
- 887401-92-5
- 英文名:
- INCB 3284
- 英文别名:
- INCB-003284;N-({1-[4-Hydroxy-4-(6-methoxy-pyridin-3-yl)-cyclohexyl]-pyrrolidin-3-ylcarbamoyl}-methyl)-3-trifluoromethyl-benzamide;Benzamide, N-[2-[[(3R)-1-[trans-4-hydroxy-4-(6-methoxy-3-pyridinyl)cyclohexyl]-3-pyrrolidinyl]amino]-2-oxoethyl]-3-(trifluoromethyl)-
- 中文名:
- INCB-3284
- 中文别名:
- CBNumber:
- CB92735525
- 分子式:
- C26H31F3N4O4
- 分子量:
- 520.54
- MOL File:
- 887401-92-5.mol
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INCB-3284化学性质
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沸点:
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703.7±60.0 °C(Predicted)
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密度:
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1.35±0.1 g/cm3(Predicted)
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储存条件:
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Store at -20°C
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溶解度:
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DMSO (Slightly), Methanol (Slightly)
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形态:
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Solid
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酸度系数(pKa):
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12.94±0.46(Predicted)
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颜色:
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Yellow to Dark Yellow
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INCB-3284性质、用途与生产工艺
INCB 3284 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 可用于急性肝功能衰竭的研究。
MCP-1-hCCR2
3.7 nM (IC
50
)
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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.
INCB-3284
上下游产品信息
上游原料
下游产品
887401-92-5, INCB-3284 相关搜索:
- C26H31F3N4O4
- 887401-92-5
- Benzamide, N-[2-[[(3R)-1-[trans-4-hydroxy-4-(6-methoxy-3-pyridinyl)cyclohexyl]-3-pyrrolidinyl]amino]-2-oxoethyl]-3-(trifluoromethyl)-
- INCB-003284
- N-({1-[4-Hydroxy-4-(6-methoxy-pyridin-3-yl)-cyclohexyl]-pyrrolidin-3-ylcarbamoyl}-methyl)-3-trifluoromethyl-benzamide