AMG 487 是一种有效的、选择性的趋化因子受体3 (CXCR3) 拮抗剂 Information AMG 487 AMG 487 is an orally active and selective CXC chemokine receptor 3 (CXCR3) antagonist that inhibits the binding of IP-10 (CXCL10) and ITAC (CXCL11) to CXCR3 with IC50 of 8.0 nM and 8.2 nM, respectively. Targets CXCR3-CXCL10 (Cell-free assay); CXCR3-CXCL11 (Cell-free assay) 8.0 nM; 8.2 nM In vitro AMG487 is the targeted blocker of chemokine receptor CXCR3 and improves inflammatory symptoms by blocking the inflammatory cycle. AMG487 significantly affects DC maturity in vitro and function leading to impaired T cell activation, inducing DCs to have characteristics similar to tolerogenic DCs. AMG487 may directly play an immunomodulatory role during DC development and functional shaping. In vivo AMG487 exhibits the antiarthritic effects in DBA/1J mice bearing collageninduced arthritis (CIA). Cell Research(from reference) Cell lines：Murine bone marrow-derived DCs (BMDCs) Concentrations：3 μM, 15 μM, 30 μM, 60 μM Incubation Time：over 6 days
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AMG 487
CAS number：473719-41-4 molecular formula：C32H28F3N5O4
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| Chinese alias | - | ||
| English alias | AMG 487 | 473719-41-4 | AMG-487 | 355CGR2CBL | CHEMBL397983 | Benzeneacetamide, N-((1R)-1-(3-(4-ethoxyphenyl)-3,4-dihydro-4-oxopyrido(2,3-d)pyrimidin-2-yl)ethyl)-N-(3-pyridinylmethyl)-4-(trifluoromethoxy)- | (R)-N-(1-(3-(4-ethoxyphenyl)-4-oxo-3,4-dihydrop | ||
| CAS number | 473719-41-4 | molecular formula | C32H28F3N5O4 |
| molecular weight | 603.59 g/mol | Exact mass | 10mM in DMSO |
| PSA | 97.200 Ų | logp | 6.334 |
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