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Naveglitazar racemate
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。
Naveglitazar racemate图片
CAS NO:916085-47-7
规格:98%
分子量:422.47
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议
20mg电议

产品介绍
Naveglitazarracemate是Naveglitazar的外消旋体。Naveglitazar是过氧化物酶体增殖物激活受体(PPAR)α-γ双重,γ显性激动剂,在动物模型具有降低葡萄糖潜力。
CAS:916085-47-7
分子式:C25H26O6
分子量:422.47
纯度:98%
存储:Store at -20°C

Background:

Naveglitazar racemate is the racemate of Naveglitazar. Naveglitazar is a nonthiozolidinedione peroxisome proliferator-activated receptor (PPAR) α-γ dual, γ-dominant agonist that has shown glucose-lowering potential in animal models and in the clinic.


Naveglitazar, a non-thiazolidinediones (TZD), functions as a potent and efficacious insulin sensitizer in rodents, possessing a novel profile that may result in an improved therapeutic agent for the treatment of type 2 diabetes and associated dyslipidemia. The extent of in vitro binding of [3H]Naveglitazar to plasma proteins is evaluated by ultracentrifugation in mouse, rat, and monkey plasma. The mean percentages±S.E.M. of protein binding of radioactivity in plasma over the concentration range of 0.1 to 1000 ng/ml after in vitro incubation at 37°C for 60 min are 99.5%±0.1% (mice), 99.6%±0.1% (rat), and 99.6%±0.3% (monkey). These results show that Naveglitazar is highly bound to plasma proteins among the species examined, and binding is independent of concentration[1].


[14C]Naveglitazar is quickly absorbed and moderately metabolized before elimination. After oral administration, 47, 31, and 62% of the radioactivity, as assessed by AUC values, are circulating as metabolites in mice, rats, and monkeys, respectively. Half-lives for Naveglitazar and radioactivity are similar within each species; however, monkeys have substantially longer half-lives in comparison to mice and rats. Naveglitazar and radioactivity are slowly cleared from the system circulation in all species evaluated[1].


[1]. Yi P, et al. The disposition and metabolism of naveglitazar, a peroxisome proliferator-activated receptor alpha-gamma dual, gamma-dominant agonist in mice, rats, and monkeys. Drug Metab Dispos. 2007 Jan;35(1):51-61.