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916085-47-7

中文名稱 916085-47-7
英文名稱 Naveglitazar (racemate)
CAS 916085-47-7
分子式 C25H26O6
分子量 422.48
MOL 文件 916085-47-7.mol
916085-47-7 結(jié)構(gòu)式 916085-47-7 結(jié)構(gòu)式

基本信息

中文別名
那格列扎 (外消旋體)
英文別名
Naveglitazar (racemate)
Benzenepropanoic acid, α-methoxy-4-[3-(4-phenoxyphenoxy)propoxy]-

物理化學(xué)性質(zhì)

沸點(diǎn)587.3±50.0 °C(Predicted)
密度1.198±0.06 g/cm3(Predicted)
儲(chǔ)存條件-20°C儲(chǔ)存
溶解度溶于二甲基亞砜
酸度系數(shù)(pKa)3.54±0.10(Predicted)

常見問(wèn)題列表

生物活性
Naveglitazar racemate (LY519818 racemate) 是 Naveglitazar 的外消旋體。Naveglitazar 是過(guò)氧化物酶體增殖物激活受體 (PPAR) α-γ 雙重,γ 顯性激動(dòng)劑,在動(dòng)物模型具有降低葡萄糖潛力。
體外研究

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 [ 3 H]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.

體內(nèi)研究

[ 14 C]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.

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