产品
编 号：F042936
分子式：C19H17NO5S
分子量：371.41
分子式：C19H17NO5S
分子量：371.41
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
5mg
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10mg
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50mg
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100mg
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结构图
CAS No: 1133819-87-0
产品详情
生物活性：
Azemiglitazone (MSDC-0602) is an orally active thiazolidinedione (TZD) -like molecule, which binds to PPARγ with low binding and activating affinity. Azemiglitazone inhibits mitochondrial pyruvate carrier (MPC), which inhibits Alzheimer’s disease and diminishes nonalcoholic steatohepatitis (NASH) caused liver injury.
体内研究：
Azemiglitazone (血液中含量 2-5 μM，口服，2-4 周) 可以提高 DIO C57BL/6 小鼠横纹肌，脂肪组织和肝脏中的胰岛素灵敏度。Azemiglitazone (血液中含量 2-5 μM，口服，2-4 周) 可以改善 DIO C57BL/6 小鼠的线粒体呼吸速率。Azemiglitazone 能够减少 HTF-C 喂养的 C57BL6/J 小鼠体内 NASH 引起的肝损伤，预防 (血液中含量为 2-5 μM，口服，共 12 周) 并逆转 (血液中含量 2-5 μM，口服，共 3 周) 星状细胞活化和纤维化。Azemiglitazone (血液中含量 2-5 μM，口服) 导致 HTF-C 喂养的 LS-Mpc2-/-C57BL6/J 小鼠体重减轻，抑制星状细胞激活，活性不受 MPC 功能的影响。Animal Model:HTF-C diet feeding C57BL6/J mice
Dosage:331 ppm MSDC-0602 potassium salt (2-5 μM Azemiglitazone in blood)
Administration:oral administration for 12 weeks (after 4 weeks of HTF-C diet) or 3 weeks (16 weeks after HTF-C diet)
Result:Induced weight loss, decreased concentrations of plasma ALT and AST and stellate cell activation.
Animal Model:HTF-C diet feeding LS-Mpc2-/-C57BL6/J mice
Dosage:331 ppm MSDC-0602 potassium salt (2-5 μM Azemiglitazone in blood)
Administration:oral administration for 12 weeks (after 4 weeks of HTF-C diet)
Result:Induced weight loss, suppressed stellate cell activation.
Animal Model:diet induced obesity C57BL/6 mice
Dosage:300 ppm MSDC-0602 (2-5 μM Azemiglitazone in blood)
Administration:oral administration for 2-4 weeks
Result:Reduced insulin concentration in plasma, increased glucose infusion rate and glucose uptake into gastrocnemius, adipose tissue, and heart.Improved mitochondrial oxygen consumption.
体外研究：
Azemiglitazone (15 μM, 4 h) 特异性的与 MPC 交联，通过与 MPC2 相互作用，抑制肝粒体中丙酮酸氧化和葡萄糖的产生。Azemiglitazone 对 PPARγ 的结合和激活亲和力低，IC50 是 18.25 μM。
Azemiglitazone (MSDC-0602) is an orally active thiazolidinedione (TZD) -like molecule, which binds to PPARγ with low binding and activating affinity. Azemiglitazone inhibits mitochondrial pyruvate carrier (MPC), which inhibits Alzheimer’s disease and diminishes nonalcoholic steatohepatitis (NASH) caused liver injury.
体内研究：
Azemiglitazone (血液中含量 2-5 μM，口服，2-4 周) 可以提高 DIO C57BL/6 小鼠横纹肌，脂肪组织和肝脏中的胰岛素灵敏度。Azemiglitazone (血液中含量 2-5 μM，口服，2-4 周) 可以改善 DIO C57BL/6 小鼠的线粒体呼吸速率。Azemiglitazone 能够减少 HTF-C 喂养的 C57BL6/J 小鼠体内 NASH 引起的肝损伤，预防 (血液中含量为 2-5 μM，口服，共 12 周) 并逆转 (血液中含量 2-5 μM，口服，共 3 周) 星状细胞活化和纤维化。Azemiglitazone (血液中含量 2-5 μM，口服) 导致 HTF-C 喂养的 LS-Mpc2-/-C57BL6/J 小鼠体重减轻，抑制星状细胞激活，活性不受 MPC 功能的影响。Animal Model:HTF-C diet feeding C57BL6/J mice
Dosage:331 ppm MSDC-0602 potassium salt (2-5 μM Azemiglitazone in blood)
Administration:oral administration for 12 weeks (after 4 weeks of HTF-C diet) or 3 weeks (16 weeks after HTF-C diet)
Result:Induced weight loss, decreased concentrations of plasma ALT and AST and stellate cell activation.
Animal Model:HTF-C diet feeding LS-Mpc2-/-C57BL6/J mice
Dosage:331 ppm MSDC-0602 potassium salt (2-5 μM Azemiglitazone in blood)
Administration:oral administration for 12 weeks (after 4 weeks of HTF-C diet)
Result:Induced weight loss, suppressed stellate cell activation.
Animal Model:diet induced obesity C57BL/6 mice
Dosage:300 ppm MSDC-0602 (2-5 μM Azemiglitazone in blood)
Administration:oral administration for 2-4 weeks
Result:Reduced insulin concentration in plasma, increased glucose infusion rate and glucose uptake into gastrocnemius, adipose tissue, and heart.Improved mitochondrial oxygen consumption.
体外研究：
Azemiglitazone (15 μM, 4 h) 特异性的与 MPC 交联，通过与 MPC2 相互作用，抑制肝粒体中丙酮酸氧化和葡萄糖的产生。Azemiglitazone 对 PPARγ 的结合和激活亲和力低，IC50 是 18.25 μM。
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