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培菲替尼氢溴酸盐  98%

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包装规格：25mg 100mg in glass bottle
产品简介：一种具有口服活性的 JAK 抑制剂，对 JAK1、JAK2、JAK3 和 Tyk2 的 IC50 值分别为 3.9、5.0、0.7 和 4.8 nM。
靶点：JAK3:0.7 nM (IC50); JAK1:3.9 nM (IC50); Tyk2:4.8 nM (IC50); JAK2:5 nM (IC50).
体外研究：Peficitinib hydrobromide (0-100 nM; 3 days) inhibits IL-2-induced T cell proliferation in a concentration-dependent manner. Peficitinib hydrobromide (10-1000 nM) inhibits IL-2-induced STAT5 phosphorylation in a concentration-dependent manner with a mean IC50 of 124 nM in rat whole blood, and inhibits STAT5 phosphorylation with a mean IC50 of 127 nM in human lymphocytes.
体内研究：Peficitinib hydrobromide (1-30 mg/kg; p.o.; once daily for 24 days) shows dose-dependent efficacy both in prophylactic and therapeutic dosing regimens in an adjuvant-induced arthritis rat model.
细胞实验：Cell Proliferation Assay Cell Line:Splenocytes from male Lewis rats Concentration:0-100 nM Incubation Time:3 days Result:Inhibited IL-2-induced T cell proliferation in a concentration-dependent manner with an IC50 of 10 nM.
动物实验：Animal Model: Seven-weeks-old female Lewis rats, adjuvant-induced arthritis (AIA) model. Dosage:1, 3, 10, and 30 mg/kg. Administration:Oral administration, once daily for 24 days. Result:Significantly inhibited the increase in paw volume at doses of 1 mg/kg or greater with an ED50 value of 2.7 mg/kg (95% confidence interval: 1.5–4.2 mg/kg). Significantly reduced the bone destruction score at 10 mg/kg or greater and almost fully ameliorated both paw swelling and bone destruction scores at 30 mg/kg.
保存条件：-20°C
注意事项：1、为了您的安全和健康，请穿实验服并戴一次性手套操作。 2、以上信息仅做参考交流之用。

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