916085-47-7
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- CAS号:
- 916085-47-7
- 英文名:
- Naveglitazar (racemate)
- 英文别名:
- Naveglitazar (racemate);Benzenepropanoic acid, α-methoxy-4-[3-(4-phenoxyphenoxy)propoxy]-
- 中文名:
- 916085-47-7
- 中文别名:
- 化合物 T12185;那格列扎 (外消旋体)
- CBNumber:
- CB13175557
- 分子式:
- C25H26O6
- 分子量:
- 422.48
- MOL File:
- 916085-47-7.mol
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916085-47-7化学性质
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沸点:
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587.3±50.0 °C(Predicted)
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密度:
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1.198±0.06 g/cm3(Predicted)
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储存条件:
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Store at -20°C
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溶解度:
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Soluble in DMSO
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酸度系数(pKa):
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3.54±0.10(Predicted)
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916085-47-7性质、用途与生产工艺
Naveglitazar racemate (LY519818 racemate) 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。
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.
[
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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.
916085-47-7
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916085-47-7, 916085-47-7 相关搜索:
- 化合物 T12185
- 那格列扎 (外消旋体)
- 916085-47-7
- Benzenepropanoic acid, α-methoxy-4-[3-(4-phenoxyphenoxy)propoxy]-
- Naveglitazar (racemate)