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Dabigatran Etexilate

甲磺酸达比加群酯,BIBR-1048,BIBR 1048,BIBR1048

Dabigatran etexilate是口服活性的dabigatran原药，是可逆的直接凝血酶抑制剂（DTI），Ki为4.5 nM。

目录号
EY0451
EY0451
EY0451
纯度
99.29%
99.29%
99.29%
规格
5 mg
10 mg
50 mg
原价
620
915
3600
售价
620
915
3600
库存
现货
现货
现货
订购
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  • 生物活性

    Dabigatran Etexilate is the prodrug of dabigatran, a potent, nonpeptidic small molecule that specifically and reversibly inhibits both free and clot-bound thrombin by binding to the active site of the thrombin molecule.

  • 体外研究

  • 体内研究

  • 激酶实验

  • 细胞实验

  • 动物实验

  • 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 A的Km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] Wienen W, et al. Thromb Haemost, 2007, 98(1), 155-162.
    [2] Maegdefessel, L. et al. 2010. Vasc Health Risk Manag. 6 : 339-349.
    [3] Walenga, J.M. and Adiguzel, C. 2010. Int. J. Clin. Pract. 64(7): 956-967.
    [4] Verma, A.K. 2010. Med. J. Aust. 192(7): 407-412.

    分子式
    C34H41N7O5    		 分子量
    627.73    		 CAS号
    211915-06-9    		 储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂（常温）
    		 DMSO
    ≥120 mg/mL    		 Water
    <1 mg/mL    		 Ethanol
    12 mg/mL

    体内溶解度

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

    NCT01976507 Atrial Fibrillation|Atrial Flutter Drug: dabigatran etexilate mesylate Vanderbilt University Medical Center|Boehringer Ingelheim Phase 4 2013-10-01 2017-02-21
    NCT02426229 Scleroderma|Interstitial Lung Disease Drug: dabigatran etexilate Medical University of South Carolina|National Institute of Arthritis and Musculoskeletal and Skin Diseases (NIAMS) Phase 1 2016-02-01 2017-03-22
    NCT02173717 Healthy Drug: Dabigatran etexilate|Drug: Rifampicin Boehringer Ingelheim Phase 1 2009-06-01 2014-06-24
    NCT01711853 Renal Insufficiency, Chronic Drug: Dabigatran Etexilate Boehringer Ingelheim Phase 1 2012-10-01 2015-01-09
    NCT00844415 Venous Thromboembolism Drug: dabigatran etexilate Boehringer Ingelheim Phase 2 2009-06-01 2014-06-03
    NCT01083732 Venous Thromboembolism Drug: dabigatran etexilate Boehringer Ingelheim Phase 2 2010-03-01 2016-11-02
    NCT01184989 Arthroplasty, Replacement,|Prevention of Venous Thromboembolism,|Moderate Renal Impairment (CrCl 30-50 mL/Min) Drug: Dabigatran etexilate Boehringer Ingelheim Phase 4 2010-08-01 2014-06-03
    NCT02171481 Healthy Drug: Dabigatran etexilate polymorph II|Drug: Dabigatran etexilate polymorph I Boehringer Ingelheim Phase 1 2008-05-01 2014-06-20
    NCT02170675 Healthy Drug: Dabigatran etexilate|Drug: Ketoconazole Boehringer Ingelheim Phase 1 2009-06-01 2014-06-20
    NCT03070171 Healthy Drug: dabigatran etexilate Boehringer Ingelheim Phase 1 2017-03-01 2017-03-20
    NCT01290757 Healthy Drug: Dabigatran etexilate|Drug: Dabigatran etexilate Boehringer Ingelheim Phase 1 2011-01-01 2014-05-08
    NCT02945020 Healthy Drug: Dabigatran etexilate mesylate|Drug: Odalasvir (ODV)|Drug: Simeprevir (SMV) Janssen Research & Development, LLC Phase 1 2016-11-01 2016-12-11
    NCT01546883 Atrial Fibrillation Drug: Dabigatran etexilate (Pradaxa) University of Utah Phase 4 2012-02-01 2015-09-10
    NCT02197416 Venous Thromboembolism|Secondary Prevention Drug: dabigatran etexilate Boehringer Ingelheim Phase 3 2014-09-01 2017-03-20
    NCT02170571 Hepatic Insufficiency Drug: Dabigatran etexilate Boehringer Ingelheim Phase 1 2005-07-01 2014-06-20
    NCT02348723 Atrial Fibrillation Drug: Warfarin|Drug: Dabigatran Etexilate 150mg Boehringer Ingelheim Phase 4 2015-04-01 2017-03-07
    NCT02171000 Healthy Drug: BIBR 1048 MS Boehringer Ingelheim Phase 1 2005-04-01 2014-06-20
    NCT02223260 Venous Thromboembolism Drug: dabigatran Boehringer Ingelheim Phase 2 2014-09-01 2016-07-28

    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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