916085-47-7
中文名称 | 916085-47-7 |
---|---|
中文同义词 | 那格列扎 (外消旋体);化合物 T12185 |
英文名称 | Naveglitazar (racemate) |
英文同义词 | Naveglitazar (racemate);Benzenepropanoic acid, α-methoxy-4-[3-(4-phenoxyphenoxy)propoxy]- |
CAS号 | 916085-47-7 |
分子式 | C25H26O6 |
分子量 | 422.48 |
EINECS号 | |
相关类别 | |
Mol文件 | 916085-47-7.mol |
结构式 | ![]() |
916085-47-7 性质
沸点 | 587.3±50.0 °C(Predicted) |
---|---|
密度 | 1.198±0.06 g/cm3(Predicted) |
储存条件 | Store at -20°C |
溶解度 | 溶于二甲基亚砜 |
酸度系数(pKa) | 3.54±0.10(Predicted) |
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.
[ 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.