Peficitinib

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Peficitinib (ASP-015K, JNJ-54781532) 是一种有效的 JAK 抑制剂，对 JAK1 和 JAK3 的 IC50 值分别为 3.9 和 0.7 nM；抑制体外 IL-2 依赖性 T 细胞增殖以及体外和离体 STAT5 磷酸化；在佐剂诱导的大鼠关节炎模型中，剂量依赖性地抑制骨质破坏和爪肿胀。

Peficitinib (ASP-015K, JNJ-54781532) is a potent JAK inhibitor with IC50s of 3.9 and 0.7 nM for JAK1 and JAK3 respectively; inhibits IL-2-dependent T cell proliferation in vitro and STAT5 phosphorylation in vitro and ex vivo; dose-dependently suppresses bone destruction and paw swelling in an adjuvant-induced arthritis model in rats; orally bioactive.Rheumatoid Arthritis Phase 3 Clinical.

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. 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.

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.

ASP-015K | JNJ-54781532

Angiogenesis

JAK

JAK

Inflammation/Immunology

Rheumatoid Arthritis

944118-01-8

326.3929

C18H22N4O2

>98% (HPLC)

DMSO: ≥ 60 mg/mL

C1C2CC3CC(C2)(CC1C3NC4=C5C=CNC5=NC=C4C(=O)N)O

1H-Pyrrolo[2,3-b]pyridine-5-carboxamide, 4-[(5-hydroxytricyclo[3.3.1.13,7]dec-2-yl)amino]-, stereoisomer

(-20℃)

With Ice Pack

≥ 2 years