Home > IκB/IKK & > Bardoxolone Methyl

Bardoxolone Methyl

甲基巴多索隆,RTA 402,RTA402,RTA-402,TP-155,NSC 713200,NSC-713200,NSC713200,CDDO Methyl Ester

Bardoxolone Methyl是一种IKK抑制剂,具有强效的促凋亡和抗炎活性。

目录号
EY0595
EY0595
EY0595
EY0595
纯度
99.27%
99.27%
99.27%
99.27%
规格
5 mg
10 mg
50 mg
100 mg
原价
288
489
890
1400
售价
288
489
890
1400
库存
现货
现货
现货
现货
订购
订购
订购
订购
订购
订购
  • 生物活性

    Bardoxolone Methyl is an IKK inhibitor, showing potent proapoptotic and anti-inflammatory activities. Phase 3.

  • 体外研究

  • 体内研究

  • 激酶实验

  • 细胞实验

    ~5 μM

  • 动物实验

    ~60 mg/kg 口服给药

  • 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] Honda T, et al. J Med Chem. 2000, 43(22), 4233-4246.
    [2] Prevention of prostate cancer with oleanane synthetic triterpenoid CDDO-Me in the TRAMP mouse model of prostate cancer By Gao, Xiaohua; Deeb, Dorrah; Liu, Yongbo; Arbab, Ali S.; Divine, George W.; Dulchavsky, Scott A.; Gautam, Subhash C.From Cancers (Basel). 2011; 3(3): 3353-3369

    分子式
    C32H43NO4
    分子量
    505.69
    CAS号
    218600-53-4
    储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂(常温)
    DMSO
    20 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
    NCT03068130 Pulmonary Hypertension Drug: Bardoxolone methyl Reata Pharmaceuticals, Inc. Phase 3 2017-04-01 2017-03-06
    NCT00529438 Advanced Solid Tumors|Lymphoid Malignancies Drug: Bardoxolone methyl Reata Pharmaceuticals, Inc. Phase 1 2006-04-01 2014-11-04
    NCT03019185 Alport Syndrome Drug: Placebo Oral Capsule|Drug: Bardoxolone Methyl Reata Pharmaceuticals, Inc. Phase 2|Phase 3 2017-03-02 2017-03-15
    NCT02657356 Connective Tissue Disease-Associated Pulmonary Arterial Hypertension Drug: Placebo capsules|Drug: Bardoxolone methyl capsules Reata Pharmaceuticals, Inc. Phase 3 2016-09-01 2017-03-09
    NCT01461161 Healthy Volunteers Drug: bardoxolone methyl Reata Pharmaceuticals, Inc. Phase 1 2011-10-01 2012-03-30
    NCT01053936 Renal Insufficiency, Chronic|Diabetes Mellitus, Type 2 Drug: Bardoxolone methyl (amorphous dispersion) Reata Pharmaceuticals, Inc. Phase 2 2010-01-01 2012-06-12
    NCT00811889 Chronic Kidney Disease|Type 2 Diabetes|Diabetic Nephropathy Other: Placebo|Drug: Bardoxolone Methyl (RTA 402) Reata Pharmaceuticals, Inc. Phase 2 2009-04-01 2012-06-12
    NCT02036970 Pulmonary Arterial Hypertension|Pulmonary Hypertension Drug: Bardoxolone methyl|Drug: Placebo Reata Pharmaceuticals, Inc. Phase 2 2014-05-01 2017-03-08
    NCT00664027 Diabetic Nephropathy Drug: RTA 402 (Bardoxolone Methyl) Reata Pharmaceuticals, Inc. Phase 2 2008-04-01 2012-11-29
    NCT01351675 Renal Insufficiency, Chronic|Diabetes Mellitus, Type 2 Drug: Placebo|Drug: Bardoxolone Methyl: 20 mg Reata Pharmaceuticals, Inc. Phase 3 2011-06-01 2014-04-28
    NCT01549769 Renal Insufficiency, Chronic|Diabetes Mellitus, Type 2 Drug: Bardoxolone Methyl Reata Pharmaceuticals, Inc. Phase 1 2012-04-01 2014-04-28
    NCT01563562 Hepatic Impairment|Healthy Drug: Bardoxolone Methyl Reata Pharmaceuticals, Inc. Phase 1 2012-04-01 2013-04-09
    NCT02316821 Chronic Kidney Disease|Type 2 Diabetes Drug: RTA 402|Drug: Placebo Kyowa Hakko Kirin Co., Ltd Phase 2 2014-12-01 2017-01-03
    NCT00535314 Malignant Melanoma Drug: RTA 402 Dose1|Drug: RTA 402 Dose2 Reata Pharmaceuticals, Inc. Phase 2 null 2014-10-27
    NCT00508807 Lymphoid Malignancies|Solid Tumors Drug: RTA 402 M.D. Anderson Cancer Center|Reata Pharmaceuticals, Inc. Phase 1 2006-04-01 2012-07-27
    NCT01551446 Renal Insufficiency, Chronic|Diabetes Mellitus, Type 2 Drug: Bardoxolone Methyl Reata Pharmaceuticals, Inc. Phase 1 2012-04-01 2012-11-01
    NCT00550849 Liver Disease Drug: RTA 402|Drug: RTA 402|Drug: RTA 402 Reata Pharmaceuticals, Inc. Phase 1|Phase 2 2007-04-01 2007-11-06
    NCT01503866 Healthy Drug: bardoxolone methyl Reata Pharmaceuticals, Inc. Phase 1 2011-12-01 2011-12-31
    NCT01572610 Chronic Kidney Disease|Type 2 Diabetes Drug: RTA 402 Kyowa Hakko Kirin Co., Ltd Phase 2 2012-02-01 2017-02-28
    NCT01574365 Chronic Kidney Disease|Type 2 Diabetes Drug: RTA 402 Kyowa Hakko Kirin Co., Ltd Phase 2 2012-02-01 2017-02-28
    NCT00529113 Pancreatic Neoplasms|Pancreatic Cancer Drug: Bardoxolone methyl|Drug: Bardoxolone methyl|Drug: Bardoxolone methyl|Drug: Bardoxolone methyl|Drug: Bardoxolone methyl|Drug: Bardoxolone methyl|Drug: Bardoxolone methyl|Drug: Gemcitabine|Drug: Placebo|Drug: Bardoxolone methyl Reata Pharmaceuticals, Inc. Phase 1|Phase 2 2007-09-01 2014-11-13
    NCT01655186 Renal Insufficiency, Chronic|Diabetes Mellitus, Type 2 Drug: Bardoxolone Methyl|Drug: Placebo Reata Pharmaceuticals, Inc. Phase 2 2012-09-01 2012-10-19

    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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