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Sitaxentan sodium

西他塞坦钠,TBC-11251,TBC11251,TBC 11251

Sitaxsentan钠盐(IPI 1040; TBC 11251)是内皮素A(ETA)受体拮抗剂。

目录号
EY1662
EY1662
EY1662
EY1662
纯度
99.18%
99.18%
99.18%
99.18%
规格
5 mg
10 mg
50 mg
100 mg
原价
735
1160
3320
5120
售价
735
1160
3320
5120
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

    Sitaxentan sodium is a selective endothelin A receptor (ETA) antagonist with IC50 and Ki of 1.4 nM and 0.43 nM, respectively, exhibits 7000-fold selectivity over ETB. Phase 3.

  • 体外研究

  • 体内研究

  • 激酶实验

  • 细胞实验

    0 μM -10 μM

  • 动物实验

    50 mg/kgi.v., p.o.

  • 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] Wu C, et al. J Med Chem. 1997, 40(11), 1690-1697.

    分子式
    C18H14ClN2NaO6S2
    分子量
    476.89
    CAS号
    210421-74-2
    储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂(常温)
    DMSO
    40 mg/mL
    Water
    <1 mg/mL
    Ethanol
    20 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
    NCT01204853 Hypertension, Pulmonary Drug: Sitaxentan Pfizer Phase 3 2010-08-01 2011-10-26
    NCT01445873 Pulmonary Arterial Hypertension Drug: Sitaxentan sodium Pfizer 2009-12-01 2012-05-09
    NCT01210443 Hypertension, Pulmonary Drug: Sitaxentan Pfizer Phase 3 2010-11-01 2011-11-10
    NCT00080457 Pulmonary Hypertension Drug: sitaxsentan sodium Encysive Pharmaceuticals Phase 3 2003-05-01 2007-11-08
    NCT00995566 Pulmonary Arterial Hypertension Drug: Sitaxentan sodium Pfizer 2010-04-01 2012-02-06
    NCT00303498 Diastolic Heart Failure Drug: Sitaxsentan sodium|Drug: Placebo Pfizer Phase 2 2006-03-01 2012-10-08
    NCT00981968 Healthy Drug: Sitaxentan sodium/Placebo|Drug: Sitaxentan sodium/Placebo Pfizer Phase 1 2009-09-01 2010-10-14
    NCT00811018 Pulmonary Arterial Hypertension Drug: Sitaxsentan Pfizer Phase 3 2003-03-01 2012-03-29
    NCT00034307 Pulmonary Hypertension Drug: sitaxsentan sodium ICOS-Texas Biotechnology|ICOS Corporation|Texas Biotechnology Corporation Phase 2|Phase 3 null 2005-06-23
    NCT00795639 Pulmonary Arterial Hypertension|Pulmonary Hypertension Drug: Sitaxsentan|Drug: Placebo Pfizer Phase 3 2008-12-01 2015-03-04
    NCT00796510 Pulmonary Arterial Hypertension|Pulmonary Hypertension Drug: Sitaxsentan|Drug: Sitaxsentan and Sildenafil Pfizer Phase 3 2010-07-01 2012-01-20
    NCT00796666 Pulmonary Arterial Hypertension|Pulmonary Hypertension Drug: Sitaxsentan|Drug: Sitaxsentan and Sildenafil Pfizer Phase 3 2009-05-01 2015-03-04
    NCT00810732 Chronic Kidney Disease|CRD Drug: Sitaxsentan|Drug: Nifedipine|Drug: Placebo Pfizer Phase 2 2007-05-01 2012-08-08
    NCT00744211 Heart Disease VA Office of Research and Development|Medical University of South Carolina 2008-07-01 2014-11-05
    NCT00593905 Pulmonary Arterial Hypertension|Pulmonary Hypertension|PAH WHO Group I Drug: Sitaxsentan|Drug: Bosentan, Ambrisentan West Penn Allegheny Health System|National Institutes of Health (NIH)|Baylor College of Medicine|Emory University|University of Chicago|Johns Hopkins University|Tufts Medical Center|Sir Mortimer B. Davis - Jewish General Hospital|London Health Sciences Centre|University of Maryland|University of California, San Francisco|University of Calgary|Chest Medical Associates|Columbia University|Lung Diagnostics, Ltd.|Duke University|University of California, Los Angeles|Latter Day Saints Hospital|Louisiana State University Health Sciences Center in New Orleans|Massachusetts General Hospital|Mayo Clinic|Medical College of Wisconsin|Southeastern Lung Care|Suncoast Lung Center|Children's Hospital Colorado|University Hospitals Cleveland Medical Center|University of Colorado, Denver|University of Michigan|University of Pittsburgh|University of Southern California|The University of Texas Medical Branch, Galveston|Vanderbilt University|Wayne State University|Ohio State University|University of Alabama at Birmingham|Washington University School of Medicine|Sentara Norfolk General Hospital|University of Texas Southwestern Medical Center|Bay Area Chest Physicians 2005-07-01 2012-01-20

    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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