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  • Baricitinib

    • 巴瑞克替尼;INCB 028050;LY 3009104;INCB028050;LY3009104;LY-3009104; INCB-028050
    货号: abs810404
    CAS号: 1187594-09-7
    分子式: C16H17N7O2S
    分子量: 371.42
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    货号-规格 货期 价格 数量
    abs810404-5mg 现货 ¥965.00
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    abs810404-10mg 现货 ¥1274.00
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    abs810404-50mg 现货 ¥5418.00
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    abs810404-100mg 现货 ¥7740.00
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    大包装询价
    产品描述
    描述

    Baricitinib is a selective JAK1 and JAK2 inhibitor with IC50 of 5.9 nM and 5.7 nM, ~70 and ~10-fold selective versus JAK3 and Tyk2, no inhibition to c-Met and Chk2. Phase 3.

    纯度
    >98%
    储存/保存方法
    Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
    基本信息
    别名
    巴瑞克替尼;INCB 028050;LY 3009104;INCB028050;LY3009104;LY-3009104; INCB-028050
    外观
    白色至类白色结晶性粉末
    可溶性/溶解性
    DMSO : 69 mg/mL (185.8 mM)





    生物活性
    靶点
    JAK2 ,JAK1 ,TYK2 ,JAK3
    In vitro(体外研究)
    Baricitinib inhibits IL-6–stimulated phosphorylation of the canonical substrate STAT3 (pSTAT3) and subsequent production of the chemokine MCP-1 with IC50 values of 44 nM and 40 nM, respectively, in PBMCs. Baricitinib also inhibits pSTAT3 stimulated by IL-23 with IC50 od 20 nM in isolated naive T-cells.
    In vivo(体内研究)
    Baricitinib inhibits IL-6–stimulated phosphorylation of STAT3 in whole blood with an IC50 of 128 nM. Baricitinib (10 mg/kg p.o.) is expected to inhibit JAK1/2 signaling (by ≥50%) in rats for about 8 hours. Baricitinib (10 mg/mL, p.o.) inhibits disease scores in dose-dependent manner in rats with established disease in the adjuvant arthritis model. Baricitinib treatment, compared with vehicle, inhibits the increase in hind paw volumes during the 2 weeks of treatment by 50% at a dose of 1 mg/kg and >95% at doses of 3 mg/kg or 10 mg/kg. Baricitinib treatment, compared with vehicle, also inhibits composite score of immune infiltrate, edema, and periarticular tissue appearance by 27% at a dose of 1 mg/kg, 64% at doses of 3 mg/kg and 82% at doses of 10 mg/kg in rats with established disease in the adjuvant arthritis model. Baricitinib reduces bone resorption by 15%, 61%, and 67% with increasing dose level (1, 3, and 10 mg/kg) in rats with established disease in the adjuvant arthritis model. Baricitinib (10 mg/kg, daily for 2 wk, p.o.) results in radiographic improvements with restoration of the normal architecture and appearance to the ankle and tarsals in rats with established disease in the adjuvant arthritis model. Baricitinib reduces levels of pSTAT3 in a dose- and time-dependent manner in the peripheral blood of rAIA animals. Baricitinib (10 mg/mL, p.o.) improves a composite score of joint damage by 47% in the murine CIA model. Baricitinib (10 mg/kg) reduces pannus (74%) and bone damage (78%) and improves cartilage damage (43%) and signs of inflammation (33%), resulting in a 53% improvement in an aggregate score of disease in the collagen Ab-induced arthritis (CAIA) murine model. Baricitinib (10 mg/kg) inhibits the delayed-type hypersensitivity response by 48% in both the CIA and CAIA models. Baricitinib is efficacious in active rheumatoid arthritis patients refractory to disease modifying drugs and biologics. Baricitinib preferentially inhibits JAK1 and JAK2, with 10-fold selectivity over Tyk2 and 100-fold over JAK3. The observed effects of GLPG-0634 on the ACR20, albeit in a smaller study, appear to be at least as good as that seen with tofacitinib and superior to that of baricitinib, since baricitinib only moderately affect the ACR20 values in Phase IIa clinical studies. Baricitinib has the dose-limiting side-effect of inducing anaemia which has been attributed to its effects on JAK2 but has clearly shown efficacy.
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    • 实验方法 实验条件
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