您好，欢迎来到半岛电竞官方网址 ！ [ 登录] [ 免费注册]
半岛电竞官方网址
发布求购
位置： 首页> 半岛bd体育手机客户端 库> Zaragozic Acid A
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：
Zaragozic Acid A
本半岛bd体育手机客户端 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。
Zaragozic Acid A图片
CAS NO: 142561-96-4
包装与价格：
包装 价格(元)
1mg 电议
5mg 电议

半岛bd体育手机客户端 介绍

rat liver squalene synthase inhibitor

Cas No. 142561-96-4
别名 萨拉哥酸A,Squalestatin S1
化学名 (1S,3S,4S,5R,6R,7R)-1-((4S,5R)-4-acetoxy-5-methyl-3-methylene-6-phenylhexyl)-6-(((4S,6S,E)-4,6-dimethyloct-2-enoyl)oxy)-4,7-dihydroxy-2,8-dioxabicyclo[3.2.1]octane-3,4,5-tricarboxylic acid
Canonical SMILES O[C@@H]1[C@H]([C@@]2([C@](C(O)=O)([C@H](O[C@@]1(CCC([C@H]([C@@H](CC3=CC=CC=C3)C)OC(C)=O)=C)O2)C(O)=O)O)C(O)=O)OC(/C=C/[C@H](C[C@H](CC)C)C)=O
分子式 C35H46O14
分子量 690.73
溶解度 Soluble in ethanol, methanol, DMSO, DMF
储存条件 Store at -20℃,protect from light
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
半岛bd体育手机客户端 描述

Ki: 78 pM for rat liver squalene synthase

The zaragozic acids (ZAs), which is a family of fungal metabolites containing a novel 4,6,7-trihydroxy-2,8-dioxobicyclo[3.2.1]octane-3,4,5-tricarboxylic acid core, have been independently discovered by two separate groups via screening natural product sources to discover inhibitors of squalene synthase.

In vitro: Zaragozic acid A, as well as it two analogs Zaragozic acid B and C were discovered from an unidentified sterile fungal culture, Spororniella intermedia, and Leptodontium elatius, respectively. Zaragozic acid A, B and C were reported to be three potent competitive inhibitors of rat liver squalene synthase with Ki values of 78 pM, 29 pM, and 45 pM, respectively. In addition, Zaragozic acid A, B and C could also inhibite cholesterol synthesis in Hep G2 cells [1].

In vivo: In the mouse model, zaragozic acid A was found to be an inhibitor of acute hepatic cholesterol synthesis (50% inhibitory dose of 200 μg/kg). The in-vivo inhibition of squalene synthase was accompanied by an accumulation of label from [3Hjmevalonate into farnesyl diphosphate, farnesol, as well as organic acids. In summary, these data showed the zaragozic acids were a new class of therapeutic agents with potential for the hypercholesterolemia treatment [1].

Clinical trial: Up to now, zaragozic acid A is still in the preclinical development stage.

Reference:
[1] Bergstrom JD,Kurtz MM,Rew DJ,Amend AM,Karkas JD,Bostedor RG,Bansal VS,Dufresne C,VanMiddlesworth FL,Hensens OD, et al. Zaragozic acids: a family of fungal metabolites that are picomolar competitive inhibitors of squalene synthase. Proc Natl Acad Sci U S A.1993 Jan 1;90(1):80-4.
Baidu
map