Home > RAAS & > Azilsartan Medoxomil

Azilsartan Medoxomil

阿齐沙坦酯,TAK-491,TAK 491,TAK491,

Azilsartan酯是口服活性的1型血管紧张素II受体拮抗剂，IC50为0.62 nM。

目录号
EY0518
EY0518
EY0518
纯度
99.51%
99.51%
99.51%
规格
2 mg
5 mg
10 mg
原价
668.00
990
1420
售价
668.00
990
1420
库存
现货
现货
现货
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  • 生物活性

    Azilsartan Medoxomil is a potent angiotensin II type 1 (AT1) receptor antagonist, inhibits the RAAS, with an IC50 of 2.6 nM, exhibits >10,000-fold selectivity over AT2.

  • 体外研究

  • 体内研究

  • 激酶实验

  • 细胞实验

    ~10 nM

  • 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] Ojima M, et al. J Pharmacol Exp Ther, 2011, 336(3), 801-808.
    [2] Kajiya T, Ho C, Wang J, Molecular and cellular effects of azilsartan: a new generation angiotensin II receptor blocker. J Hypertens. 2011 Dec;29(12):2476-83.
    [3] Kusumoto K, Igata H, Ojima M, Antihypertensive, insulin-sensitising and renoprotective effects of a novel, potent and long-acting angiotensin II type 1 receptor blocker, azilsartan medoxomil, in rat and dog models.

    分子式
    C30H24N4O8    		 分子量
    568.53    		 CAS号
    863031-21-4    		 储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂（常温）
    		 DMSO
    110 mg/mL    		 Water
    <1 mg/mL    		 Ethanol
    <1 mg/mL

    体内溶解度

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

    NCT02517866 Essential Hypertension|Type 2 Diabetes Mellitus Drug: Azilsartan Medoxomil Takeda Phase 4 2015-08-01 2017-01-31
    NCT02756819 Hypertension Drug: Azilsartan Medoxomil Takeda Phase 4 2016-06-01 2016-11-23
    NCT02203916 Hypertension Drug: Azilsartan medoxomil|Drug: Azilsartan medoxomil placebo Takeda Phase 3 2014-07-01 2016-10-25
    NCT01456169 Essential Hypertension Drug: Azilsartan medoxomil/placebo|Drug: Azilsartan medoxomil - chlorthalidone Takeda Phase 3 2011-10-01 2014-03-21
    NCT00818883 Essential Hypertension Drug: Azilsartan medoxomil and chlorthalidone|Drug: Azilsartan medoxomil and hydrochlorothiazide Takeda Phase 3 2009-02-01 2012-01-04
    NCT00695955 Hypertension Drug: Azilsartan medoxomil with or without add-on chlorthalidone|Drug: Azilsartan medoxomil with or without add-on hydrochlorothiazide Takeda Phase 3 2007-06-01 2011-03-24
    NCT01774591 Hypertension Drug: Azilsartan medoximil|Drug: Placebo University of Chicago|Takeda 2013-01-01 2016-01-08
    NCT01496430 Hypertension|Diabetes Drug: Placebo|Drug: Azilsartan medoxomil|Drug: Azilsartan medoxomil Takeda Phase 3 2012-01-01 2015-04-20
    NCT02480764 Essential Hypertension Drug: Azilsartan medoxomil|Drug: Valsartan|Drug: Azilsartan medoxomil Placebo|Drug: Valsartan Placebo Takeda Phase 3 2015-09-01 2016-12-14
    NCT02451150 Pediatric Hypertension Drug: Azilsartan Takeda Phase 3 2015-08-01 2016-03-08
    NCT02541669 Healthy Volunteer Drug: TAK-491|Drug: TAK-491 placebo Takeda Phase 1 2015-11-01 2016-11-29
    NCT00996281 Essential Hypertension Drug: Azilsartan medoxomil and chlorthalidone|Drug: Olmesartan medoxomil and hydrochlorothiazide Takeda Phase 3 2009-10-01 2012-10-15
    NCT01033071 Essential Hypertension Drug: Azilsartan medoxomil and chlorthalidone|Drug: Azilsartan medoxomil and chlorthalidone|Drug: Olmesartan medoxomil and hydrochlorothiazide Takeda Phase 3 2010-01-01 2012-01-04
    NCT01309828 Safety Drug: Azilsartan medoxomil and chlorthalidone|Drug: Olmesartan medoxomil and hydrochlorothiazide Takeda Phase 3 2011-03-01 2013-09-28
    NCT00591578 Hypertension Drug: Azilsartan Medoxomil|Drug: Azilsartan Medoxomil|Drug: Valsartan Takeda Phase 3 2007-12-01 2012-01-31
    NCT02791438 Pediatric Hypertension Drug: TAK-536 2.5 mg|Drug: TAK-536 5 mg Takeda Phase 3 2016-08-01 2017-03-02
    NCT00591253 Hypertension Drug: Azilsartan medoxomil|Drug: Azilsartan medoxomil|Drug: Placebo Takeda Phase 3 2007-10-01 2011-03-24
    NCT00696384 Hypertension Drug: Azilsartan medoxomil|Drug: Azilsartan medoxomil, with or without chlorthalidone and other non-angiotensin II receptor blocker antihypertensive medications.|Drug: Placebo Takeda Phase 3 2007-06-01 2011-11-29
    NCT00846365 Essential Hypertension Drug: Azilsartan medoxomil and chlorthalidone|Drug: Azilsartan medoxomil and chlorthalidone|Drug: Olmesartan medoxomil-hydrochlorothiazide Takeda Phase 3 2009-03-01 2012-02-09
    NCT03042299 Japanese Healthy Adult Male Participants Drug: TAK-536 10mg|Drug: TAK-536 10mg Takeda Phase 1 2017-02-01 2017-02-09
    NCT00760214 Hypertension Drug: Azilsartan medoxomil|Drug: Azilsartan medoxomil|Drug: Ramipril Takeda Phase 3 2008-01-01 2012-11-08

    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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