培菲替尼氢溴酸盐

Peficitinibhydrobromide
1353219-05-2

询价 1kg 起订

安徽更新日期：2024-04-12

安庆百诺医药科技有限公司

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Name	Peficitinib hydrobromide

Description	Peficitinib (ASP015K) hydrobromide 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.
Related Catalog	Signaling Pathways >> JAK/STAT Signaling >> JAK Signaling Pathways >> Epigenetics >> JAK Signaling Pathways >> Stem Cell/Wnt >> JAK Research Areas >> Inflammation/Immunology
Target	JAK3:0.7 nM (IC50) JAK1:3.9 nM (IC50) JAK2:5 nM (IC50) Tyk2:4.8 nM (IC50)
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 IC50 of 124 nM in rat whole blood, and inhibits STAT5 phosphorylation with a mean IC50 of 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 IC50 of 10 nM.
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 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.
References	[1]. Ito M, et al. A novel JAK inhibitor, peficitinib, demonstrates potent efficacy in a rat adjuvant-induced arthritis model. J Pharmacol Sci. 2017 Jan;133(1):25-33.

Molecular Formula	C18H23BrN4O2
Molecular Weight	407.30

安庆百诺医药科技有限公司是集研发、生产为一体的专业化生产医药中间体和原料药的医药化工企业，公司专门为制药公司、研发公司提供定制合成，合成研究和服务，生产医药中间体和精细化学品的制药企业和研究机构。生产基地占地50亩，配备500L到3000L各种类型反应设备以及各类检测仪器，可以提供从公斤级至吨位级的产品数量需求。公司拥有一支经验丰富的创新研发团队,研发专员来自国内各大高校，具有充沛的理论知识和实践经验。研发基地配备50L-100L的玻璃反应釜以及NMR，LC-MS，HPLC，GC等各类能够达到国际质量检验标准的检测仪器。可以满足客户从克到公斤级的高质量的产品定制。我们始终坚持“质量是企业的生命”。我们秉着“质优，诚信，共赢”理念合作，与国内外知名医药化工等多类企业建立了长期良好的合作。我们有信心会成为您的合作伙伴！安庆百诺与海内外有识之士、各界朋友，精诚合作，携手发展，共创未来。竭诚欢迎国内外客户来访指导，洽谈业务。

成立日期	(6年)
注册资本	100万
员工人数	1-10人
年营业额	￥ 300万-500万
经营模式	工厂,定制,服务
主营行业	医药中间体,原料药