INCB8761(PF-4136309)
| 中文名称 | INCB8761(PF-4136309) |
|---|---|
| 中文同义词 | 化合物PF4136309;N-(2-((S)-3-((TRANS-4-反式-4-羟基-4-(5-(嘧啶-2-基)吡啶-2-基)环己基)氨基)吡咯烷-1-基)-2-OXOETHYL)-3-(三氟甲基)苯甲酰胺 |
| 英文名称 | INCB8761(PF-4136309) |
| 英文同义词 | INCB8761(PF-4136309);NCB8761(PF-4136309);PF-04136309(INCB-8761);Benzamide, N-[2-[(3S)-3-[[trans-4-hydroxy-4-[5-(2-pyrimidinyl)-2-pyridinyl]cyclohexyl]amino]-1-pyrrolidinyl]-2-oxoethyl]-3-(trifluoromethyl)-;EOS-61910;N-(2-((S)-3-(((1r,4S)-4-hydroxy-4-(5-(pyrimidin-2-yl) yridine-2-yl)cyclohexyl)amino)pyrrolidin-1-yl)-2-oxoethyl)-3-(trifluoromethyl)benzamide;ZNSVOHSYDRPBGI-LXWOLXCRSA-N;N-(2-((S)-3-(((1R,4S)-4-HYDROXY-4-(5-(PYRIMIDIN-2-YL) |
| CAS号 | 1341224-83-6 |
| 分子式 | C29H31F3N6O3 |
| 分子量 | 568.59 |
| EINECS号 | |
| 相关类别 | G蛋白偶联受体&G蛋白;生物活性分子-API;精细化工产品 |
| Mol文件 | 1341224-83-6.mol |
| 结构式 |  |
INCB8761(PF-4136309) 性质
| 沸点 | 712.2±60.0 °C(Predicted) |
|---|---|
| 密度 | 1.40±0.1 g/cm3(Predicted) |
| 储存条件 | Keep in dark place,Inert atmosphere,Store in freezer, under -20°C |
| 溶解度 | 溶于 DMSO（至少 25 mg/ml） |
| 形态 | 固体 |
| 酸度系数(pKa) | 13.17±0.46(Predicted) |
| 颜色 | 米白色 |
| 稳定性 | 可在-20°C的DMSO中的溶液下储存长达3个月。 |
|
Human CCR2 5.2 nM (IC 50 ) |
Mouse CCR2 13 nM (IC 50 ) |
Rat CCR2 17 nM (IC 50 ) |
PF-4136309 is potent in human chemotaxis activity (IC 50 =3.9 nM) and in the whole blood assay (IC 50 =19 nM), with IC 50 of 16 and 2.8 nM in mouse and rat chemotaxis assays. PF-4136309 is potent in inhibiting CCR2 mediated signaling events such as intracellular calcium mobilization and ERK (extracellular signal-regulated kinase) phosphorylation with IC 50 values of 3.3 and 0.5 nM, respectively. In hERG patch clamp assay, PF-4136309 inhibits hERG potassium current with an IC 50 of 20 μM. PF-4136309 is not a cytochrome P450 (CYP) inhibitor, with IC 50 values of >30 μM against five major CYP isozymes CYP1A2, CYP2C9, CYP2C19, CYP2D6, and CYP3A4. Moreover, PF-4136309 is not a CYP inducer at concentrations up to 30 μM.
PF-4136309 (2 mg/kg) exhibits a moderate half-life in both species after iv administration (2.5 and 2.4 h). When administered orally, PF-4136309 (10 mg/kg) is absorbed rapidly, with peak concentration time (T max ) at 1.2 h for rats and 0.25 h for dogs. A similar half-life is observed in both species between iv dosing and po dosing. PF-4136309 is well absorbed, with an oral bioavailability of 78% in both species.
安全信息
| 海关编码 | 2933998090 |
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