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CAS No.: 2127109-84-4

Ropsacitinib Catalog No. CSN26122

Synonyms: PF-6826647;Tyk2-IN-8

PF-06826647 is a selective TYK2 inhibitor It is being tested in moderate-to-severe psoriasis in a Phase II clinical trial.

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400-920-2911

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技术信息

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].
参考文献

[1] Brian S Gerstenberger,et al. Discovery of Tyrosine Kinase 2 (TYK2) Inhibitor (PF-06826647) for the Treatment of Autoimmune Diseases. J Med Chem. 2020. 63(22), 13561-13577.
[2] Ravi Shankar P Singh,et al. Safety and Pharmacokinetics of the Oral TYK2 Inhibitor PF-06826647: A Phase I, Randomized, Double-Blind, Placebo-Controlled, Dose-Escalation Study. Clin Transl Sci. 2021. 14(2), 671-682.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.6082 mL
- 13.0409 mL
- 26.0818 mL
- 5 mM
- 0.5216 mL
- 2.6082 mL
- 5.2164 mL
- 10 mM
- 0.2608 mL
- 1.3041 mL
- 2.6082 mL

技术信息

CAS号

2127109-84-4

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C20H17N9

运输

蓝冰

分子量

383.41

别名

PF-6826647;Tyk2-IN-8

溶解度

DMSO	76.0 mg/mL (198.2 mM)
Water	Insoluble
Ethanol	Insoluble

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