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编 号：F744310
分子式：C18H23ClN4O2
分子量：362.85
分子式：C18H23ClN4O2
分子量：362.85
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CAS No: 1353219-06-3
产品详情
生物活性：
Peficitinib (ASP015K) hydrochloride is an orally active JAK inhibitor, with IC50s of 3.9, 5.0, 0.7 and 4.8 nM for JAK1, JAK2, JAK3 and Tyk2, respectively.
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.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.
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.
Peficitinib (ASP015K) hydrochloride is an orally active JAK inhibitor, with IC50s of 3.9, 5.0, 0.7 and 4.8 nM for JAK1, JAK2, JAK3 and Tyk2, respectively.
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.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.
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.
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