中文名 | WHI-P97 |
英文名 | WHI-P97 |
别名 | 化合物WHI-P97 4-(3',5'-二溴-4-羟基苯基)氨基-6,7-二甲氧基喹唑啉 |
英文别名 | WHI-P97 WHI P97 WHI-P-97 JAK3 Inhibitor I 2,6-dibromo-4-[(6,7-dimethoxyquinazolin-4-yl)amino]phenol Phenol, 2,6-dibromo-4-[(6,7-dimethoxy-4-quinazolinyl)amino]- WHI-P 974-(3',5'-DibroMo-4-hydroxyphenyl)aMino-6,7-diMethoxyquinazoline |
CAS | 211555-05-4 |
化学式 | C16H13Br2N3O3 |
分子量 | 455.1 |
密度 | 1.785 |
沸点 | 470.9±45.0 °C(Predicted) |
酸度系数 | 7.05±0.36(Predicted) |
存储条件 | -20℃ |
体外研究 | 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. |
体内研究 | 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. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.197 ml | 10.986 ml | 21.973 ml |
5 mM | 0.439 ml | 2.197 ml | 4.395 ml |
10 mM | 0.22 ml | 1.099 ml | 2.197 ml |
5 mM | 0.044 ml | 0.22 ml | 0.439 ml |
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