4-[4-(4-氟苯基)-2-(4-硝基苯基)-1H-咪唑-5-基]吡啶
中文名称 | 4-[4-(4-氟苯基)-2-(4-硝基苯基)-1H-咪唑-5-基]吡啶 |
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中文同义词 | 4-[4-(4-氟苯基)-2-(4-硝基苯基)-1H-咪唑-5-基]吡啶 |
英文名称 | PD 169316 |
英文同义词 | 4-[5-(4-fluorophenyl)-2-(4-nitrophenyl)-1H-iMidazol-4-yl]pyridine;Pyridine, 4-[4-(4-fluorophenyl)-2-(4-nitrophenyl)-1H-iMidazol-5-yl]-;PD169316/PD-169316;4-[4-(4-Fluorophenyl)-2-(4-nitrophenyl)-1H-imidazol-5-yl]pyridine;4-[4-(4-Fluorophenyl)-2-(4-nitrophenyl)-1H-imidazol-5-yl]pyridine PD 169316;PD 169316 4-[4-(4-Fluorophenyl)-2-(4-nitrophenyl)-1H-imidazol-5-yl]pyridine;PD 169316, >=98%;PD 169316, >97% |
CAS号 | 152121-53-4 |
分子式 | C20H13FN4O2 |
分子量 | 360.34 |
EINECS号 | 200-256-5 |
相关类别 | 信号转导通路激酶抑制剂;小分子抑制剂;活性分子;小分子抑制剂,天然产物;Inhibitors;Aromatics;Heterocycles;Intermediates & Fine Chemicals;Pharmaceuticals;Protein Kinase Inhibitors and Activators |
Mol文件 | 152121-53-4.mol |
结构式 |
4-[4-(4-氟苯基)-2-(4-硝基苯基)-1H-咪唑-5-基]吡啶 性质
沸点 | 583.1±50.0 °C(Predicted) |
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密度 | 1.354±0.06 g/cm3(Predicted) |
储存条件 | 2-8°C |
溶解度 | 二甲基亚砜:>10mg/mL |
酸度系数(pKa) | 9.09±0.10(Predicted) |
形态 | 固体 |
颜色 | 浅橙色 |
Target | Value |
TGF-β
() | |
Activin A
() | |
Enterovirus71
() | |
p38 MAPK
(Cell-free assay) | 89 nM |
PD169316 (10 μM) inhibits TGFβ and Activin A, but not BMP4 signaling in CaOV3 cells. PD169316 (0.2-20 μM) inhibits TGFβ-induced Smad2 nuclear translocation, Smad7 mRNA induction, and reporter gene activity in CaOV3 cells. PD169316 (10 μM) shows a significantly increased rate of proliferation in Nestin knockdown cells, and can rescue the effect of Nestin knockdown on cell viability in the absence of EGF. PD169316 significantly inhibits p38 MAP kinase activity with no significant change in ERK activity in PC12 cells. PD169316 (10 μM) blocks apoptosis induced by trophic factor withdrawal in differentiated PC12 cells.PD169316 (10 μM, 30 min) selectively inhibits the kinase activity of the phosphorylated p38 without hindering upstream kinases to phosphorylate p38. Increased phospho p-38 levels in the presence of PD169316 are most likely due to blockade of negative feedback loop of dephosphorylation of p38 MAPK by MAPK phosphatases.
Western Blot Analysis
Cell Line: | Ishikawa PRB or PRA cells. |
Concentration: | 10 μM. |
Incubation Time: | 30 min. |
Result: | Did not inhibit MEKK1-induced p38 phosphorylation. |
PD169316 (1 mg/kg, intramuscular injection every day for 14 consecutive days) shows antiviral activity in a suckling mouse model.
Animal Model: | EV71-challenged suckling mouse model (7-day-old Kunming mice). |
Dosage: | 1 mg/kg. |
Administration: | Intramuscular injection every day for 14 consecutive days. |
Result: | Showed antiviral activity. |
安全信息
危险品标志 | Xn |
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危险类别码 | 22-37/38-41 |
安全说明 | 26-39 |
危险品运输编号 | UN 2811 6.1/PG 3 |
WGK Germany | 3 |
海关编码 | 2933399990 |
更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
---|---|---|---|---|---|
2024/01/16 | P2532 | PD 169316 PD 169316 | 152121-53-4 | 10mg | 355元 |
2024/01/16 | S5183 | 4-[4-(4-氟苯基)-2-(4-硝基苯基)-1H-咪唑-5-基]吡啶 PD 169316 | 152121-53-4 | 5mg | 570.25元 |