4-[4-(4-氟苯基)-2-(4-硝基苯基)-1H-咪唑-5-基]吡啶

生物活性靶点体外研究体内研究 4-[4-(4-氟苯基)-2-(4-硝基苯基)-1H-咪唑-5-基]吡啶试剂级价格

CAS号:152121-53-4
英文名:PD 169316
中文名:4-[4-(4-氟苯基)-2-(4-硝基苯基)-1H-咪唑-5-基]吡啶
CBNumber:CB7497465
分子式:C20H13FN4O2
分子量:360.34
MOL File:152121-53-4.mol

4-[4-(4-氟苯基)-2-(4-硝基苯基)-1H-咪唑-5-基]吡啶化学性质

沸点 :583.1±50.0 °C(Predicted)
密度 :1.354±0.06 g/cm3(Predicted)
储存条件 :2-8°C
溶解度 :DMSO: >10mg/mL
酸度系数(pKa) :9.09±0.10(Predicted)
形态 :solid
颜色 :light orange

安全信息

危险品标志 :Xn
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

4-[4-(4-氟苯基)-2-(4-硝基苯基)-1H-咪唑-5-基]吡啶性质、用途与生产工艺

生物活性 PD 169316 是一种有效的、细胞可渗透的选择性 p38 MAP kinase 抑制剂，IC50值为89 nM。 PD169316 可消除 TGFbeta 和 Activin A 引发的信号传导。 PD169316对 Enterovirus71 具有抗病毒活性。
靶点
Target Value
TGF-β
()
Activin A
()
Enterovirus71
()
p38 MAPK
(Cell-free assay) 89 nM

体外研究

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.

体内研究

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.