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奥美沙坦

更新时间:2024-01-02 18:00:19

奥美沙坦结构式
奥美沙坦结构式
品牌特惠专场
常用名 奥美沙坦 英文名 Olmesartan
CAS号 144689-24-7 分子量 446.502
密度 1.3±0.1 g/cm3 沸点 738.3±70.0 °C at 760 mmHg
分子式 C24H26N6O3 熔点 186-188ºC
MSDS 中文版 美版 闪点 400.3±35.7 °C

 奥美沙坦用途


Olmesartan 是血管紧张素II受体 (AT1R) 拮抗剂,常用于治疗高血压。

 奥美沙坦名称

中文名 奥美沙坦
英文名 olmesartan
中文别名 奥美沙坦酸 | 4-(1-羟基-1-甲基乙基)-2-丙基-1-[2'-(四唑-5-基)苯基]苯基]甲基咪唑-5-羧酸
英文别名 更多

 奥美沙坦生物活性

描述 Olmesartan 是血管紧张素II受体 (AT1R) 拮抗剂,常用于治疗高血压。
相关类别
体内研究 反复给予奥美沙坦(1 mg/kg,2 mg/kg,po)剂量依赖性地降低SHR中的平均动脉血压(MAP),而在10周内对体重和食物摄入没有显着影响[1]。奥美沙坦(5 mg/kg/d,po)和Hyd治疗可使小鼠的收缩压降低至相同程度。奥美沙坦治疗通过超声心动图,心脏重量,心肌细胞的横截面积和基因表达来评估心脏肥大。奥美沙坦治疗逆转了Ren-Tg小鼠ACE2和Mas受体的基因表达减少,并抑制了NADPH氧化酶(Nox)4表达和活性氧的增强[2]。
动物实验 将7周龄雄性自发性高血压大鼠(SHR)分成5组,随意喂食高脂肪饮食(HFD)(60%kcal作为脂肪)。通过胃管饲法每天一次用载体(1%黄蓍胶溶液),替米沙坦(1mg / kg),替米沙坦(2mg / kg),奥美沙坦(1mg / kg)或奥美沙坦(2mg / kg)治疗SHR。治疗超过4周后,在意识状态下测量平均动脉血压24小时。
参考文献

[1]. Yanagihara H, et al. Effects of telmisartan and olmesartan on insulin sensitivity and renal function in spontaneously hypertensive rats fed a high fat diet. J Pharmacol Sci. 2016 Jul;131(3):190-7.

[2]. Tanno T, et al. Olmesartan Inhibits Cardiac Hypertrophy in Mice Overexpressing Renin Independently of Blood Pressure: Its Beneficial Effects on ACE2/Ang(1-7)/Mas Axis and NADPH Oxidase Expression. J Cardiovasc Pharmacol. 2016 Jun;67(6):503-9.

[3]. Komiya H, et al. Sleep/wakefulness behaviors in mice during pregnancy and pregnancy-associated hypertensive mice. Sleep. 2018 Mar 1;41(3).

 奥美沙坦物理化学性质

密度 1.3±0.1 g/cm3
沸点 738.3±70.0 °C at 760 mmHg
熔点 186-188ºC
分子式 C24H26N6O3
分子量 446.502
闪点 400.3±35.7 °C
精确质量 446.206635
PSA 129.81000
LogP 3.72
外观性状 白色固体
蒸汽压 0.0±2.6 mmHg at 25°C
折射率 1.671
储存条件 -20°C Freezer

 奥美沙坦安全信息

危害码 (欧洲) Xi
危险品运输编码 NONH for all modes of transport
RTECS号 NI4014100
海关编码 2921590090

 奥美沙坦海关

海关编码 2921590090
中文概述 2921590090. 其他芳香多胺及衍生物及它们的盐. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:30.0%
申报要素 品名, 成分含量, 用途
Summary 2921590090. other aromatic polyamines and their derivatives; salts thereof. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:30.0%

 奥美沙坦文献4

更多文献
Structure-response relationship in electrospray ionization-mass spectrometry of sartans by artificial neural networks.

J. Chromatogr. A. 1438 , 123-32, (2016)

Quantitative structure-property relationship (QSPR) methods are based on the hypothesis that changes in the molecular structure are reflected in changes in the observed property of the molecule. Artif...

Synergistic, cytotoxic and apoptotic activities of olmesartan with NF-κB inhibitor against HeLa human cell line.

Toxicol. Mech. Methods 25 , 614-21, (2015)

Over expression of renin-angiotensin system (RAS) and nuclear factor-kappaB (NF-κB) has a major role in many cancers. It has been suggested that some angiotensin receptor blockers (ARBs) could reduce ...

Linear mixed-effects model of QTc prolongation for olmesartan medoxomil.

J. Clin. Pharmacol. , doi:10.1002/jcph.572, (2015)

 奥美沙坦英文别名

4-(2-Hydroxy-2-propanyl)-2-propyl-1-{[2'-(1H-tetrazol-5-yl)-4-biphenylyl]methyl}-1H-imidazole-5-carboxylic acid
Olmesartan Acid
MFCD00914967
Olmesartan
5-(2-hydroxypropan-2-yl)-2-propyl-3-[[4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]imidazole-4-carboxylic acid
1H-Imidazole-5-carboxylic acid, 4-(1-hydroxy-1-methylethyl)-2-propyl-1-[[2'-(1H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl]-
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