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首页 / 抑制剂/激动剂 / G蛋白偶联受体/G蛋白 / 血管紧张素受体 / Olmesartan/奥美沙坦

Olmesartan/奥美沙坦 {[allProObj[0].p_purity_real_show]}

货号：A891128 同义名： RNH-6270; CS 088

Olmesartan is an antagonist of angiotensin II receptor, working as an antihypertensive agent.

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Olmesartan/奥美沙坦 化学结构 CAS号：144689-24-7
Olmesartan/奥美沙坦 化学结构
CAS号：144689-24-7
Olmesartan/奥美沙坦 3D分子结构
CAS号：144689-24-7
Olmesartan/奥美沙坦 化学结构 CAS号：144689-24-7
Olmesartan/奥美沙坦 3D分子结构 CAS号：144689-24-7
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Olmesartan/奥美沙坦 纯度/质量文件 产品仅供科研

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Olmesartan/奥美沙坦 生物活性

靶点

  • AT1 receptor
描述 Angiotensin II is an important hormonal effector and end-product of the renin-angiotensin system. After binding to its endogenous receptor sites, it causes widespread vasoconstriction and a subsequent increase in blood pressure. [3]. Olmesartan (RNH-6270) is an angiotensin II receptor (AT1R) antagonist used to treat high blood pressure.[4] Olmesartan (0.7-5 mM; 24, 48 and 72 h) inhibits the growth of HeLa cells as a concentration- and time-dependent mode. [5]. A single i.v. administration of olmesartan (0.01-0.03mg/kg) produced a dose-related inhibition that reached a maximum within 30 min after dosing,followed by a gradual decline over 8h in rats.[6]. Repeated dosing of olmesartan (1 mg/kg, 2 mg/kg, p.o.) dose-dependently decreases mean arterial blood pressure (MAP) in SHR without significant influence on body weight and food intake during 10 weeks. Olmesartan (5 mg/kg/d, p.o.) and hydralazine treatments lower systolic blood pressure to the same degree in mice. Olmesartan treatment inhibits cardiac hypertrophy, evaluated by echocardiography, heart weight, cross-sectional area of cardiomyocytes, and gene expression. Olmesartan treatment reverses decreased gene expressions of ACE2 and Mas receptor of Ren-Tg mice and inhibits enhanced NADPH oxidase (Nox)4 expression and reactive oxygen species. [7].
作用机制 AT1R can homodimerize and heterodimerize with other G-protein coupled receptors (GPCR), altering the receptor signaling properties. Olmesartan,biased AT1R agonists preferentially activate the β-arrestin signaling pathway.[2].

Olmesartan/奥美沙坦 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT01415466 Healthy Phase 1 Completed - Korea, Republic of ... 展开 >> Yonsei University Health System (Yuhs) Seoul, Korea, Republic of 收起 <<
NCT00185120 Hypertension Phase 4 Completed - United States, Alabama ... 展开 >> Mobile, Alabama, United States, 36693 United States, California Memorial Research Medical Center Long Beach, California, United States, 90806 National Research Institute Los Angeles, California, United States, 90057 Clinical Trials Research Roseville, California, United States, 95661 Apex Research Institute Santa Ana, California, United States, 92705 Orange County Research Center Tustin, California, United States, 92780 Westlake Medical Center Westlake Village, California, United States, 91361 United States, Florida Clinical Research of South Florida Coral Gables, Florida, United States, 33134 The Greater Fort Lauderdale Heart Group Research Fort lauderdale, Florida, United States, 33308 SFBC International Miami, Florida, United States, 33142 CLIRECO, Inc. Tamarac, Florida, United States, 33321 United States, Indiana Midwest Institute for Clinical Research Indianapolis, Indiana, United States, 46260 United States, Kansas Heartland Research Associates Wichita, Kansas, United States, 67207 United States, Maine Androscoggin Cardiology Research Auburn, Maine, United States, 04210 United States, North Carolina Internal Medicine Associates of Charlotte Charlotte, North Carolina, United States, 28211 Piedmont Medical Research Associates Winston-salem, North Carolina, United States, 27103 United States, Ohio The Lindner Clinical Trial Center Cincinnati, Ohio, United States, 45319 United States, Rhode Island Omega Medical Research Warwick, Rhode Island, United States, 02886 United States, Tennessee Volunteer Research Group, University of Tennessee Med. Ctr. Knoxville,, Tennessee, United States, 37920 United States, Texas Punzi Medical Center Carrollton, Texas, United States, 75006 收起 <<
NCT01028534 Obstructive Sleep Apnea ... 展开 >> Hypertension 收起 << Not Applicable Completed - Japan ... 展开 >> Kirigaoka Tsuda Hospital Kitakyushu, Japan Kyoto University Hospital Kyoto, Japan 收起 <<

Olmesartan/奥美沙坦 参考文献

[1]Yanagisawa H et al. Nonpeptide angiotensin II receptor antagonists: synthesis, biological activities, and structure-activity relationships of imidazole-5-carboxylic acids bearing alkyl, alkenyl, and hydroxyalkyl substituents at the 4-position and Their Related Compounds J. Med. Chem., 1996, 39 (1), pp 323-338

[2] Takanobu Takezako,et al. Current Topics in Angiotensin II Type 1 Receptor Research: Focus on Inverse Agonism, Receptor Dimerization and Biased Agonism, Pharmacol Res. 2017 Sep;123:40-50

[3]Kim Chilman-Blair,et al. Olmesartan, an AT1-selective antihypertensive agent. Drugs Today (Barc).2003 Oct;39(10):745-61.

[4] 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.

[5]Bakhtiari E, et al. Synergistic, cytotoxic and apoptotic activities of olmesartan with NF-κB inhibitor against HeLa human cell line. Toxicol Mech Methods.2015;25(8):614-21.

[6] H Koike,et al. In vitro and in vivo pharmacology of olmesartan medoxomil, an angiotensin II type AT1 receptor antagonist, J Hypertens Suppl. 2001 Jun;19(1):S3-14.

[7]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 Ca-rdiovasc Pharmacol. 2016 Jun;67(6):503-9.

Olmesartan/奥美沙坦 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.24mL

0.45mL

0.22mL

11.20mL

2.24mL

1.12mL

22.40mL

4.48mL

2.24mL

Olmesartan/奥美沙坦 技术信息

CAS号144689-24-7
分子式C24H26N6O3
分子量 446.5
SMILES Code O=C(O)C1=C(N=C(N1CC2=CC=C(C=C2)C3=CC=CC=C3C4=NN=NN4)CCC)C(O)(C)C
MDL No. MFCD00914967
别名 RNH-6270; CS 088; CS-866; Votum; Olmetec; Benicar
运输蓝冰
InChI Key VTRAEEWXHOVJFV-UHFFFAOYSA-N
Pubchem ID 158781
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Sealed in dry, store in freezer, under -20°C
溶解方案 请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用； 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶
方案一
方案二

Tags: Olmesartan | RNH-6270;CS 088;CS-866;Votum;Olmetec;Benicar | Angiotensin Receptor | AmBeed-信号通路专用抑制剂 | Olmesartan/奥美沙坦 纯度/质量文件 | Olmesartan/奥美沙坦 生物活性 | Olmesartan/奥美沙坦 临床数据 | Olmesartan/奥美沙坦 参考文献 | Olmesartan/奥美沙坦 实验方案 | Olmesartan/奥美沙坦 技术信息

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