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Baricitinib

巴瑞克替尼,LY3009104,INCB028050,LY 3009104,INCB 028050,LY-3009104,INCB-028050

Baricitinib是JAK1和JAK2抑制剂,IC50分别为5.9 nM和5.7 nM,比对JAK3和Tyk2的抑制性高70倍和10倍,对c-Met和Chk2无活性。

目录号
EY0830
EY0830
EY0830
纯度
99.14%
99.14%
99.14%
规格
2 mg
5 mg
10 mg
原价
536.00_
860
1080
售价
536.00_
860
1080
库存
现货
现货
现货
订购
订购
订购
订购
订购
订购
  • 生物活性

    Baricitinib (LY3009104, INCB028050) is a selective JAK1 and JAK2 inhibitor with IC50 of 5.9 nM and 5.7 nM in cell-free assays, ~70 and ~10-fold selective versus JAK3 and Tyk2, no inhibition to c-Met and Chk2.

  • 体外研究

  • 体内研究

  • 激酶实验

  • 细胞实验

  • 动物实验

    10 mg/mL口服

  • 不同实验动物依据体表面积的等效剂量转换表(数据来源于FDA指南)

    动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 AKm系数


    例如,已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法:将88 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到该药物用于大鼠的等效剂量44 mg/kg。


  • 参考文献

    [1] Fridman JS, et al. J Immunol, 2010, 184(9), 5298-5307.

    分子式
    C16H17N7O2S
    分子量
    371.42
    CAS号
    1187594-09-7
    储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂(常温)
    DMSO
    74 mg/mL
    Water
    <1 mg/mL
    Ethanol
    <1 mg/mL

    体内溶解度

  • Clinical Trial Information ( data from http://clinicaltrials.gov )

    NCT Number Conditions Interventions Sponsor/Collaborators Phases Start Date Last Updated
    NCT02340104 Healthy Volunteers Drug: Baricitinib|Drug: [^13C4D3^15N]-baricitinib Eli Lilly and Company Phase 1 2015-01-01 2015-03-01
    NCT01968057 Healthy Volunteers Drug: Baricitinib|Drug: Ciclosporin Eli Lilly and Company Phase 1 2013-10-01 2014-01-08
    NCT01870388 Liver Diseases|Hepatic Insufficiency Drug: Baricitinib Eli Lilly and Company Phase 1 2013-06-01 2013-09-10
    NCT01925144 Healthy Volunteers Drug: Baricitinib|Drug: Omeprazole Eli Lilly and Company Phase 1 2013-10-01 2013-11-21
    NCT02263911 Healthy Volunteers Drug: Baricitinib Eli Lilly and Company Phase 1 2014-11-01 2015-01-05
    NCT03026504 Arteritis, Giant Cell Drug: Baricitinib Matthew J Koster|Eli Lilly and Company|Mayo Clinic Phase 2 2017-02-01 2017-01-19
    NCT01924299 Healthy Volunteers Drug: Baricitinib|Drug: Ketoconazole|Drug: Fluconazole Eli Lilly and Company Phase 1 2013-08-01 2013-11-21
    NCT01859078 Healthy Volunteers Drug: Baricitinib|Drug: Digoxin Eli Lilly and Company Phase 1 2013-05-01 2013-08-23
    NCT01896726 Healthy Volunteers Drug: Baricitinib|Drug: Microgynon Eli Lilly and Company Phase 1 2013-07-01 2013-10-18
    NCT02708095 Systemic Lupus Erythematosus Drug: Baricitinib|Drug: Placebo Eli Lilly and Company Phase 2 2016-03-01 2017-03-23
    NCT01937026 Healthy Volunteers Drug: Baricitinib|Drug: Probenecid Eli Lilly and Company Phase 1 2013-09-01 2013-12-03
    NCT02759731 Chronic Graft vs Host Disease|Chronic Graft-Versus-Host Disease Drug: Baricitinib National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) Phase 1|Phase 2 2016-04-08 2017-03-08
    NCT02265705 Rheumatoid Arthritis Drug: Baricitinib|Drug: Placebo Eli Lilly and Company Phase 3 2014-10-01 2016-07-01
    NCT01910311 Healthy Volunteers Drug: Baricitinib|Drug: Rifampicin Eli Lilly and Company Phase 1 2013-08-01 2013-10-30
    NCT01960140 Healthy Volunteers Drug: Baricitinib|Drug: Simvastatin Eli Lilly and Company Phase 1 2013-10-01 2014-01-08
    NCT02576938 Atopic Dermatitis Drug: Baricitinib|Drug: Placebo|Drug: Triamcinolone (Optional) Eli Lilly and Company Phase 2 2016-02-01 2017-03-14
    NCT01885078 Rheumatoid Arthritis Drug: Baricitinib|Drug: Placebo Eli Lilly and Company Phase 3 2013-06-01 2017-03-22
    NCT01683409 Diabetic Kidney Disease Drug: baricitinib|Drug: Placebo Eli Lilly and Company|Incyte Corporation Phase 2 2012-08-01 2015-01-16
    NCT01721044 Rheumatoid Arthritis Drug: Placebo|Drug: Baricitinib Eli Lilly and Company Phase 3 2013-01-01 2014-09-29
    NCT01721057 Rheumatoid Arthritis Drug: Placebo|Drug: Baricitinib Eli Lilly and Company Phase 3 2012-12-01 2015-02-19
    NCT01490632 Psoriasis|Skin Diseases|Skin Diseases, Papulosquamous Drug: Placebo|Drug: LY3009104 Eli Lilly and Company|Incyte Corporation Phase 2 2011-12-01 2014-11-25
    NCT01710358 Rheumatoid Arthritis Drug: Placebo|Drug: Adalimumab|Drug: Baricitinib Eli Lilly and Company Phase 3 2012-10-01 2016-05-13
    NCT01711359 Rheumatoid Arthritis Drug: Baricitinib|Drug: Methotrexate|Drug: Placebo|Drug: Folic Acid Eli Lilly and Company Phase 3 2012-11-01 2015-09-24
    NCT01299285 Healthy Volunteers Drug: LY3009104 Eli Lilly and Company Phase 1 2011-02-01 2011-04-06
    NCT02758613 Healthy Drug: LY3009104|Drug: Placebo Eli Lilly and Company Phase 1 2016-05-01 2016-08-25

    注:以上所有数据均来自公开文献,并不保证对所有实验均有效,数据仅供参考。

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