Peficitinib (ASP015K) hydrobromide 是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。
| 生物活性 | Peficitinib (ASP015K) hydrobromide is an orally activeJAKinhibitor, withIC50s of 3.9, 5.0, 0.7 and 4.8 nM forJAK1,JAK2,JAK3andTyk2, respectively[1]. |
| IC50& Target[1] | JAK3 0.7 nM (IC50) | JAK1 3.9 nM (IC50) | Tyk2 4.8 nM (IC50) | JAK2 5 nM (IC50) |
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体外研究
(In Vitro) | Peficitinib hydrobromide (0-100 nM; 3 days) inhibits IL-2-induced T cell proliferation in a concentration-dependent manner[1].
Peficitinib hydrobromide (10-1000 nM) inhibits IL-2-induced STAT5 phosphorylation in a concentration-dependent manner with a mean IC50of 124 nM in rat whole blood, and inhibits STAT5 phosphorylation with a mean IC50of 127 nM in human lymphocytes[1].
Cell Proliferation Assay[1] | 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 IC50of 10 nM. |
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体内研究
(In Vivo) | 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[1].
| Animal Model: | Seven-weeks-old female Lewis rats, adjuvant-induced arthritis (AIA) model[1] | | 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 ED50value 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. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
