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Macitentan

马西替坦,ACT-064992,ACT064992,ACT 064992

Macitentan(ACT064992)是口服活性的，非肽类ETA和ETB受体拮抗剂，可能可作用于特发性肺纤维化和肺动脉高压。

目录号
EY0539
EY0539
EY0539
EY0539
纯度
99.27%
99.27%
99.27%
99.27%
规格
1 mg
5 mg
10 mg
50 mg
原价
230
520
750
1200
售价
230
520
750
1200
库存
现货
现货
现货
现货
订购
订购
订购
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  • 生物活性

    Macitentan is an orally active, non-peptide, dual ETA/ETB (endothelin) receptor antagonist with IC50 of 0.5 nM/391 nM.

  • 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] Iglarz M, et al. J Pharmacol Exp Ther, 2008, 327(3), 736-745.
    [2] Bolli MH, Boss C, Binkert C, Buchmann S, Bur D, Hess P, Iglarz M, Meyer S, Rein J, Rey M, Treiber A, Clozel M, Fischli W, Weller T. The Discovery of N-[5-(4-Bromophenyl)-6-[2-[(5-bromo-2-pyrimidinyl)oxy]ethoxy]-4-pyrimidinyl]-N'-propylsulfamide (Macitentan), an Orally Active, Potent Dual Endothelin Receptor Antagonist. J Med Chem. 2012 Aug 16.
    [3] Kim SJ, Kim JS, Kim SW, Yun SJ, He J, Brantley E, Fan D, Strickner P, Lehembre F, Regenass U, Fidler IJ. Antivascular therapy for multidrug-resistant ovarian tumors by macitentan, a dual endothelin receptor antagonist. Transl Oncol. 2012 Feb;5(1):39-47.

    分子式
    C19H20Br2N6O4S    		 分子量
    588.27    		 CAS号
    441798-33-0    		 储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂（常温）
    		 DMSO
    100 mg/mL    		 Water
    <1 mg/mL    		 Ethanol
    <1 mg/mL

    体内溶解度

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

    NCT02651272 Pulmonary Hypertension|Sickle Cell Disease Drug: macitentan Boston University|Actelion Phase 1 2015-07-01 2017-03-15
    NCT01841762 Pulmonary Arterial Hypertension Drug: Macitentan Actelion Phase 3 2013-04-01 2016-06-08
    NCT02254954 Glioblastoma Drug: Macitentan in combination with RT and TMZ Actelion Phase 1 2014-10-01 2016-11-01
    NCT01739400 Pulmonary Arterial Hypertension Drug: Macitentan 10 mg tablet, once daily. Actelion Phase 3 2013-09-01 2017-03-22
    NCT01847014 Pulmonary Arterial Hypertension Drug: Macitentan Actelion Phase 3 2013-09-01 2016-06-08
    NCT02310672 Pulmonary Arterial Hypertension Drug: Macitentan Actelion Phase 4 2015-06-01 2017-01-16
    NCT02060721 Chronic Thromboembolic Pulmonary Hypertension Drug: Macitentan Actelion Phase 2 2015-02-01 2017-02-15
    NCT02081690 Pulmonary Arterial Hypertension Drug: Macitentan Actelion Phase 3 2014-03-01 2016-02-26
    NCT01743001 Pulmonary Arterial Hypertension Drug: Macitentan 10 mg|Drug: Placebo Actelion Phase 3 2013-05-01 2016-12-21
    NCT02021292 Chronic Thromboembolic Pulmonary Hypertension Drug: Macitentan|Drug: Placebo Actelion Phase 2 2014-08-01 2016-10-18
    NCT01474122 Digital Ulcers Drug: Macitentan 3 mg|Drug: Macitentan 10 mg|Drug: Placebo Actelion Phase 3 2011-12-01 2016-11-22
    NCT01474109 Systemic Sclerosis|Ulcers Drug: macitentan 3mg|Drug: macitentan 10mg|Drug: placebo Actelion Phase 3 2011-12-01 2015-01-02
    NCT00903331 Idiopathic Pulmonary Fibrosis Drug: ACT-064992 (macitentan)|Drug: Placebo Actelion Phase 2 2009-05-01 2014-01-02
    NCT01499251 Glioblastoma Drug: Phase 1 Dose Escalation|Drug: Phase 1b|Drug: Ancillary Study Actelion Phase 1 2012-01-01 2016-05-04
    NCT02893176 Lung Transplant Rejection Drug: macitentan|Drug: placebo (for macitentan) University of California, Los Angeles Phase 4 2016-09-01 2016-09-01
    NCT01346930 Idiopathic Pulmonary Fibrosis Drug: Macitentan Actelion Phase 2 2011-07-01 2014-09-02
    NCT02382016 Portopulmonary Hypertension Drug: Macitentan|Other: Placebo Actelion Phase 4 2015-06-01 2016-12-06
    NCT02126943 Pulmonary Arterial Hypertension Drug: Opsumit (macitentan) Actelion 2014-04-01 2017-01-31
    NCT00667823 Pulmonary Arterial Hypertension Drug: Macitentan Actelion Phase 3 2008-10-01 2016-11-18
    NCT02112487 Pulmonary Arterial Hypertension Drug: Macitentan Actelion Phase 3 2014-06-01 2016-11-18
    NCT02932410 Pulmonary Arterial Hypertension Drug: Macitentan|Other: Standard-of-care Actelion Phase 3 2017-06-30 2017-03-17
    NCT02554903 Pulmonary Hypertension Drug: Macitentan 10mg|Drug: Placebo sugar pill Actelion Phase 2 2015-12-01 2016-10-06
    NCT02070991 Pulmonary Hypertension Drug: Macitentan|Drug: Placebo Actelion Phase 2 2014-07-01 2017-02-16

    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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