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Bosentan

伯森坦,柏森坦,Ro 47-0203,Benzenesulfonamide

Bosentan 是一种 endothelin (ET) receptor 拮抗剂，其作用于 ET-A 和 ET-B 的 Ki 分别为 4.7 nM 和 95 nM。

目录号
EY1707
EY1707
EY1707
纯度
99.68%
99.68%
99.68%
规格
50 mg
100 mg
500 mg
原价
550
998
2760
售价
550
998
2760
库存
现货
现货
现货
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  • 生物活性

    Bosentan is an endothelin (ET) receptor antagonist for ET-A and ET-B with Ki of 4.7 nM and 95 nM, respectively.

  • 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] Gutsch, G., et al.: Cardiovasc. Drugs Ther., 10, 717 (1996)
    [2] Krum, H., et al.: N. Engl. J. Med., 338, 784 (1998)
    [3] Weber, C., et al.: Clin Pharmacol. Ther., 60, 124 (1996)

    分子式
    C27H29N5O6S    		 分子量
    551.61    		 CAS号
    147536-97-8    		 储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂（常温）
    		 DMSO
    92 mg/mL    		 Water
    <1 mg/mL    		 Ethanol
    2 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
    NCT00319267 Pulmonary Arterial Hypertension Drug: Bosentan Actelion Phase 3 2005-05-01 2016-05-23
    NCT01447550 Thromboangiitis Obliterans Drug: Bosentan Hospital Universitario Getafe 2009-01-01 2016-08-15
    NCT01223352 Pulmonary Arterial Hypertension Drug: bosentan Actelion Phase 3 2011-03-01 2016-06-02
    NCT01662037 Congenital Heart Defects|Functional Single Ventricle Drug: Bosentan Shanghai Jiao Tong University School of Medicine Phase 2 2010-01-01 2012-08-07
    NCT01425229 VA Drug Interactions [VA Drug Interaction] Drug: Bosentan Gerd Mikus|Heidelberg University 2011-06-01 2015-07-07
    NCT00595049 Hypertension, Pulmonary Drug: bosentan Actelion Phase 4 2006-05-01 2015-04-28
    NCT00319020 Pulmonary Arterial Hypertension Drug: Bosentan Actelion Phase 3 2005-08-01 2016-06-02
    NCT01184404 Congenital Heart Disease Drug: Bosentan Berto J Bouma|Academisch Medisch Centrum - Universiteit van Amsterdam (AMC-UvA) 2011-09-01 2015-12-21
    NCT01721564 Pulmonary Arterial Hypertension Drug: Bosentan Prof David S Celermajer|Royal Prince Alfred Hospital, Sydney, Australia 2006-04-01 2016-10-18
    NCT02317679 Port-wine Stains Drug: Bosentan|Device: Pulsed dye laser (PDL) Centre Hospitalier Universitaire de Nice Phase 2 2014-04-01 2014-12-15
    NCT00391443 Idiopathic Pulmonary Fibrosis Drug: Bosentan|Drug: Placebo Actelion Phase 3 2007-02-01 2015-09-09
    NCT01738542 Peripheral Arterial Disease Drug: Bosentan|Drug: Antiaggregant therapy|Drug: Statins|Drug: Antihypertensive therapy Hospital Universitario Getafe 2009-04-01 2012-11-28
    NCT02480335 Scleroderma, Systemic Drug: bosentan University Medical Center Groningen|Actelion Phase 4 2015-06-01 2015-06-19
    NCT00926627 Sarcoidosis|Pulmonary Hypertension Drug: bosentan|Drug: placebo Daniel Doberer|Medical University of Vienna Phase 2 2009-04-01 2016-09-14
    NCT00077584 Digital Ulcers|Systemic Sclerosis Drug: Bosentan 62.5 mg|Drug: Bosentan 125 mg|Drug: Placebo Actelion Phase 3 2003-10-01 2016-10-26
    NCT02377271 Ischemic Optic Neuropathy Drug: bosentan|Drug: placebo University Hospital, Grenoble Phase 3 2015-03-01 2015-02-24
    NCT00082186 Hypertension, Pulmonary Drug: bosentan Actelion Phase 4 2003-07-01 2010-02-11
    NCT01827059 Pulmonary Arterial Hypertension|Congenital Heart Disease Drug: Bosentan|Drug: Placebo Academisch Medisch Centrum - Universiteit van Amsterdam (AMC-UvA) Phase 2 2013-10-01 2015-12-21
    NCT00637065 Pulmonary Hypertension|Interstitial Lung Disease|Idiopathic Pulmonary Fibrosis|Nonspecific Interstitial Pneumonia Drug: Bosentan|Drug: Placebo Royal Brompton & Harefield NHS Foundation Trust|Actelion Phase 4 2008-04-01 2008-03-10
    NCT00679068 Pulmonary Hypertension Drug: Bosentan Azienda Ospedaliera Universitaria di Bologna Policlinico S. Orsola Malpighi Phase 4 2008-05-01 2015-08-19

    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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