Ropsacitinib
产品说明书
 |
同义名 : | PF-06826647; Tyk2-IN-8; PF-6826647; compound 10 |
| CAS号 : | 2127109-84-4 | |
| 货号 : | A1275148 | |
| 分子式 : | C20H17N9 | |
| 纯度 : | 99%+ | |
| 分子量 : | 383.41 | |
| MDL号 : | MFCD32197240 | |
| 存储条件： |
Pure form Sealed in dry, 2-8°C In solvent -20°C:3-6个月-80°C:12个月 |
|
| 溶解度 : | - | |
| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 描述 | Tyrosine kinase 2 (TYK2) is a member of the JAK kinase family that regulates signal transduction downstream of receptors for the IL-23/IL-12 pathways and type I interferon family, where it pairs with JAK2 or JAK1, respectively[1]. PF-06826647 is a selective TYK2 inhibitor. It has been tested in moderate-to-severe psoriasis in a Phase II clinical trial. PF-06826647 was absorbed rapidly, with a median Tmax of 2 hours in the fasted state. The mean terminal half-lives (t1/2) for the 3 and 10 mg groups were 3.6 and 6.0 hours, respectively. For doses of 30 mg and above, the mean t1/2 ranged from 16.3 to 38.8 hours. The AUC from time zero extrapolated to infinite time (AUCinf) and Cmax increased in a greater than dose-proportional manner at PF-06826647 doses of 3-10 mg, and in a dose-proportional manner at doses of 400-1,600 mg. However, increases in AUCinf and Cmax were less than dose-proportional at doses of 10-400 mg. Variability in exposure based on the geometric coefficient of variation ranged from 25% to 67% for AUCinf and from 25% to 62% for Cmax[2]. | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
|
1 mM 5 mM 10 mM |
2.61mL 0.52mL 0.26mL |
13.04mL 2.61mL 1.30mL |
26.08mL 5.22mL 2.61mL |
| 参考文献 |
|---|