4-(3',5'-二溴-4-羟基苯基)氨基-6,7-二甲氧基喹唑啉
| 中文名称 | 4-(3',5'-二溴-4-羟基苯基)氨基-6,7-二甲氧基喹唑啉 |
|---|---|
| 中文同义词 | 4-(3',5'-二溴-4-羟基苯基)氨基-6,7-二甲氧基喹唑啉;化合物WHI-P97;2,6-二溴-4-((6,7-二甲氧基喹唑啉-4-基)氨基)苯酚;4-(3',5'-二溴-4-羟基苯基)氨基-6,7-二甲氧基喹唑啉;WHI-P97,JAK-3抑制剂 |
| 英文名称 | WHI-P97 |
| 英文同义词 | WHI-P 974-(3',5'-DibroMo-4-hydroxyphenyl)aMino-6,7-diMethoxyquinazoline;2,6-dibromo-4-[(6,7-dimethoxyquinazolin-4-yl)amino]phenol;JAK3 Inhibitor I USP/EP/BP;Phenol, 2,6-dibromo-4-[(6,7-dimethoxy-4-quinazolinyl)amino]-;WHI-P-97;WHI P97;WHI-P97;Janus kinase,JAK,airway,Inhibitor,WHIP97,eosinophil recruitment,WHI-P97,inhibit,ovalbumin challenge,WHI P97,ovalbumin-sensitized,WHI-P-97 |
| CAS号 | 211555-05-4 |
| 分子式 | C16H13Br2N3O3 |
| 分子量 | 455.1 |
| EINECS号 | |
| 相关类别 | 蛋白酪氨酸激酶;标准品 |
| Mol文件 | 211555-05-4.mol |
| 结构式 |  |
4-(3',5'-二溴-4-羟基苯基)氨基-6,7-二甲氧基喹唑啉 性质
| 沸点 | 470.9±45.0 °C(Predicted) |
|---|---|
| 密度 | 1.785 |
| 储存条件 | Store at -20°C |
| 溶解度 | DMSO：5.88 mg/mL（12.92 mM；需要超声波）H2O：< 0.1 mg/mL（不溶） |
| 形态 | 粉末 |
| 酸度系数(pKa) | 7.05±0.36(Predicted) |
| Target | Value |
|
JAK3
() |
WHI-P97 inhibits the translocation of 5-lipoxygenase (5-LO) from the nucleoplasm to the nuclear membrane and consequently 5-LO-dependent leukotriene (LT) synthesis after IgE receptor/FcεRI crosslinking by >90% at low micromolar concentrations.WHI-P97 (30 μM) stantially reduces the IgE/antigen-induced LTC4 release from mast cells.
WHI-P97 is very well tolerated in mice, with no signs of toxicity at dose levels ranging from 5 μg/kg to 50 mg/kg, and LD 10 is not reached at a 50 mg/kg dose level when administered as a single i.p. or i.v. bolus dose.WHI-P97 (i.v. injection; 40 mg/kg; single dose) has an elimination half-life (t 1/2 ) of 58.9 min and systemic clearance (CL) of 891 ml/h/kg in CD-1 mice and a t 1/2 of 84.2 min and CL of 1513 ml/h/kg in BALB/c mice. The values for AUC and C max are 107.3 μM and 296.7 μM, respectively, in CD-1 mice. And the IC 50 values are 58.4 μM and 212.7 μM, respectively, in BALB/c mice. The large volume of distribution are 322 ml/kg in CD-1 mice and 415 ml/kg in BALB/c mice.WHI-P97 (intraperitoneal injection; 40 mg/kg; 24 days) prevents ovalbumin-sensitized mice the development of airway hyper-responsiveness to methacholine in a dose-dependent fashion in mice. WHI-P97 inhibits the eosinophil recruitment to the airway lumen after the ovalbumin challenge in a dose-dependent fashion.
| Animal Model: | BALB/c mouse model of allergic asthma |
| Dosage: | 40 mg/kg |
| Administration: | intraperitoneal injection; 24 days |
| Result: | Showed promising biological activity in a mouse model of allergic asthma at nontoxic dose levels. |