您好,欢迎来到化工原料网! [登录] [免费注册]
化工原料网
位置:首页 > 产品库 > Olmesartan medoxomil
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
Olmesartan medoxomil
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Olmesartan medoxomil图片
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
25mg电议
50mg电议
100mg电议
200mg电议

产品介绍
Olmesartan medoxomil 是一种有效的选择性血管紧张素 AT1 受体抑制剂,IC50 为 66.2 μM。

Animal experiment:

Mice[3]10 to 12-week old male db/db diabetic mice with background strain C57BL/KsJ and their age-matched non-diabetic lean control mice (C57BL) are used.10 non-diabetic control mice and 10 diabetic mice are fed with placebo (0.5% sodium CMC/saline solution), and 10 diabetic mice are fed with 20 mg/kg Olmesartan (MB5704) by daily gavage for 12 weeks. Mice are monitored for blood glucose, body weight and urine output every two weeks. After treatment, mice are euthanized and trunk blood is collected and is centrifuged to obtain plasma which is aliquoted and stored at -80℃. Kidney tissues are removed from mice. For protein extraction slices of the kidney tissue are frozen in liquid nitrogen, and stored at -80℃. Other parts of the kidney tissue are fixed with 4% paraformaldehyde and embedded in paraffin for immunostaining.

产品描述

Olmesartan medoxomil, the medoxomil ester of olmesartan, is novel and oral antagonist of angiotensin II TYPE-1 receptor (AT1receptor) with an inhibition constant IC50of 33 nmol/L. Through oral administration, olmesartan medoxomil is rapidly absorbed by the gastrointestinal tract converting to its active metabolite olmesartan, whose inhibition constant IC50towards AT1receptor is 8 nmol/L. The esterification of olmesartan with medoxomil moiety is just to improve its water solubility (from 4.5% to 28.6%). Olmesartan medoxomil is used for the treatment of hypertension, in which olmesartan dose-dependently reduces the blood pressure through arterial vasodilation and reducing sodium retention.

Reference

[1].HR Brunner. The new oral angiotensin II antagonist olmesartan medoxomil: a concise overview. Journal of Human Hypertension (2002) 16 (Suppl 2), S13-S16
[2].Shailesh T. Prajapati, Hitesh H. Bulchandani, Dashrath M. Patel, Suresh K. Dumaniya and Chhaganbhai N. Patel. Formulation and evaluation of liquisolid compacts for olmesartan medoxomil. Journal of Drug Delivery 2013.