Sitaxsentan钠盐(IPI 1040; TBC 11251)是内皮素A(ETA)受体拮抗剂。
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.
0 μM -10 μM
50 mg/kgi.v., p.o.
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。
[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
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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