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奥美沙坦酯, 1 型血管紧张素 II 受体拮抗剂

血管紧张素受体拮抗剂
  • CAS编号: 144689-63-4
  • 分子式: C29H30N6O6
  • 分子量: 558.59
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库存信息

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货号 (SKU) 包装规格 是否现货 价格 数量
O408446-1ml
1ml 现货 Stock Image
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Compound libraries (12333)

基本描述

英文别名 1H-Imidazole-5-carboxylic acid, 4-(1-hydroxy-1-methylethyl)-2-propyl-1-[[2'-(2H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl]-, (5-methyl-2-oxo-1,3-dioxol-4-yl)methyl ester
规格或纯度 Moligand™, 10mM in DMSO
英文名称 Olmesartan Medoxomil
生化机理 奥美沙坦酯(CS-866)是一种选择性血管紧张素 II 1 型(AT(1))受体拮抗剂,用于治疗高血压。
储存温度 -80℃储存
运输条件 超低温冰袋运输
作用类型 拮抗剂
作用机制 1 型血管紧张素 II 受体拮抗剂
产品介绍

Olmesartan Medoxomil水解产物为Olmesartan,是一种选择性AT1亚型血管紧缩素II受体拮抗剂。An angiotensin II receptor antagonist

Information

Olmesartan Medoxomil Olmesartan Medoxomil (CS-866) is a selective angiotensin II type 1 (AT(1)) receptor antagonist, used in the treatment of high blood pressure.
In vitro

Olmesartan Medoxomil significantly reduces liver hydroxyproline content, the mRNA expression of collagen alpha1(I) and alpha-smooth muscle actin (alpha-SMA), and plasma levels of transforming growth factor-beta1 (TGF-beta1). Olmesartan Medoxomil is a pro-drug containing an ester moiety that, after oral administration, is rapidly cleaved to release the active form Olmesartan (RNH-6270). Olmesartan is a highly potent, competitive and selective All AT1 receptor antagonist with almost no antagonistic activity on AT2 and AT4 receptors.

In vivo

Olmesartan produces a rapid and long-lasting inhibition of All-induced pressor responses in conscious rats. Oralolmesartan medoxomil also inhibits All-pressor response but onset of the action is slower compared with intravenous administration. Olmesartan Medoxomil exhibits dose-dependent antihypertensive effects in several rat and dog models, with the most marked effects seen in high plasma renin models, when compared with normal or low renin types. Olmesartan medoxomil exhibits, beside antihypertensive effects, beneficial effects in animal models of various types of nephrosis and heart failure, and anti-atherogenic effects in hyperlipidaemic animals. Olmesartan Medoxomil dose-dependently ameliorates the colonic histopathological and biochemical injuries in rats, an effect that is comparable or even better than that of the standard Sulfasalazine. Olmesartan medoxomil significantly reduces the induction of hypoxic cor pulmonale not only on echocardiographical observations but also in brain natriuretic peptide (BNP) in chronic hypoxic rats, TGF-beta and endothelin gene expressions in molecular studies.
Cell Data

cell lines:

Concentrations:

Incubation Time:

Powder Purity:≥99%

产品属性

ALogP 3.8

关联靶点(人)

SLCO1B1 Tchem 溶质载体有机阴离子转运蛋白家族成员1B1(Solute carrier organic anion transporter family member 1B1) (2 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
SLCO1B3 Tchem 溶质载体有机阴离子转运蛋白家族成员1B3(Solute carrier organic anion transporter family member 1B3) (2 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
AGTR1 Tclin 1型血管紧张素II受体(Type-1 angiotensin II receptor) (1 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)

名称和识别符

分子类型 小分子
Isomeric SMILES CCCC1=NC(=C(N1CC2=CC=C(C=C2)C3=CC=CC=C3C4=NNN=N4)C(=O)OCC5=C(OC(=O)O5)C)C(C)(C)O
分子量 558.59
Reaxy-Rn 12388067
Reaxys-RN link address https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=12388067&ln=

化学和物理性质

熔点 180-182°C

安全和危险性(GHS)

象形图 GHS08,   GHS07
信号词 Danger
危险声明

H319: 引起严重眼睛刺激

H302: 吞食有害

H312: 皮肤接触有害

H332: 吸入有害

H360: 可能损害生育力或未出生的孩子

预防措施声明

P261: 避免吸入灰尘/烟雾/气体/雾/蒸汽/喷雾

P305+P351+P338: 如进入眼睛:用水小心冲洗几分钟。如戴隐形眼镜并可方便地取出,取出隐形眼镜。继续冲洗。

P280: 戴防护手套/穿防护服/戴防护眼罩/戴防护面具。

P302+P352: 如皮肤沾染:用水充分清洗。

P321: 特殊处理(请参阅此标签上的...)。

P405: 密闭存放

P501: 将内容物/容器处理到。。。

P264: 处理后要彻底洗手。

P271: 仅在室外或通风良好的地方使用。

P270: 使用本产品时,请勿进食、饮水或吸烟。

P304+P340: 如误吸入:将人转移到空气新鲜处,保持呼吸舒适体位。

P362+P364: 脱掉沾污的衣服,清洗后方可重新使用。

P330: 漱口

P203: 使用前,获取、阅读并遵守所有安全说明。

P264+P265: 处理后彻底洗手[和…]。不要触摸眼睛。

P301+P317: 如果被吞咽:请寻求医疗帮助。

P318: 如果暴露或担心,请就医。

P317: 寻求紧急医疗救助。

P337+P317: 如果眼睛刺激持续:寻求医疗帮助。

RTECS NI4014200
Merck Index 6839

质检证书(CoA,COO,BSE/TSE 和分析图谱)

C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:

溶液计算器