855527-92-3
基本信息
N-[(1R)-1-[3-(4-Ethoxyphenyl)-3,4-dihydro-4-oxopyrido[2,3-d]pyrimidin-2-yl]ethyl]-4-fluoro-N-(3-pyridinylmethyl)-3-(trifluoromethyl)benzeneacetamide
Benzeneacetamide, N-[(1R)-1-[3-(4-ethoxyphenyl)-3,4-dihydro-4-oxopyrido[2,3-d]pyrimidin-2-yl]ethyl]-4-fluoro-N-(3-pyridinylmethyl)-3-(trifluoromethyl)-
物理化学性质
| 沸点 | 752.5±70.0 °C(Predicted) |
| 密度 | 1.32±0.1 g/cm3(Predicted) |
| 储存条件 | -20°C储存 |
| 溶解度 | DMSO:100.0(Max Conc. mg/mL);165.1(Max Conc. mM) |
| 酸度系数(pKa) | 4?+-.0.11(Predicted) |
| 形态 | 粉末 |
| 颜色 | Light yellow to yellow |
安全数据
| 危险性符号(GHS) |  GHS07 |
| 警示词 | 警告 |
| 危险性描述 | H315-H319 |
| 防范说明 | P264-P280-P302+P352-P337+P313-P305+P351+P338-P362+P364-P332+P313 |
常见问题列表
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[ 125 I]CXCL10-CXCR3 1.5 nM (Ki, in CXCR3-CHO cell membranes) |
[ 125 I]CXCL11-CXCR3 3.2 nM (Ki, in CXCR3-CHO cell membranes) |
BI-74330 demonstrates potent inhibition of [ 125 I]CXCL11 specific binding to membranes prepared from transfected CHO cells expressing CXCR3 (CXCR3-CHO) (K i =3.6 nM). NBI-74330 is 12- and 3.5-fold more potent than CXCL9 (K i =45.2 nM) and CXCL10 (K i =12.5 nM), respectively, at inhibiting [ 125 I]CXCL11 binding to CXCR3-CHO cell membranes. NBI-74330 inhibits calcium mobilization in response to CXCL11 and CXCL10 with an IC 50 value of 7 nM for both ligands used at their EC 80 concentrations (1 nM for CXCL11 and 30 nM for CXCL10). NBI-74330 specifically inhibits CXCR3-mediated calcium mobilization. NBI-74330 also dose-dependently inhibits CXCL11-induced [ 35 S]GTPγS binding in membranes of cells endogenously expressing CXCR3 (H9 cells, IC 50 value 5.5 nM). BI-74330 inhibits CXCL11-induced chemotaxis in these cells with an IC 50 of 3.9 nM. NBI-74330 (30-300 nm, 1-10 μM) produces concentration-dependent, parallel rightward shifts of the CXCL11 E/[A] curve with no significant change in the E/[A] curve maximal response.
NBI-74330 (100 mg/kg) results in the formation of an N-oxide metabolite, also an antagonist of CXCR3, in mice. Mice treated with 100 mg/kg NBI-74330 (in 1% Na Doc in 0.5% 400Cp Methylcellulose) result in serum concentrations of approximately 1 μM. This concentration is sufficient to fully block the CXCR3 receptor in vivo.