伊罗替罗

伊罗替罗化学性质

沸点 :596.3±50.0 °C(Predicted)
密度 :1.708
储存条件 :Sealed in dry,Room Temperature
溶解度 :DMSO:84.0(Max Conc. mg/mL);172.43(Max Conc. mM)
DMF:30.0(Max Conc. mg/mL);61.58(Max Conc. mM)
Ethanol:63.5(Max Conc. mg/mL);130.35(Max Conc. mM)
Ethanol:PBS (pH 7.2) (1:1):0.5(Max Conc. mg/mL);1.03(Max Conc. mM)
形态 :A crystalline solid
酸度系数(pKa) :3.16±0.32(Predicted)
颜色 :White to light yellow

伊罗替罗性质、用途与生产工艺

生物活性 Eprotirome (KB2115) 是肝脏选择性甲状腺激素受体 (thyroid hormone receptor, TR) 激动剂。KB2115 对 TRβ 的亲和力略高于 TRα。Eprotirome 降低了低密度脂蛋白 (LDL) 胆固醇的浓度，可用于血脂异常和肥胖症的研究。
靶点

Thyroid hormone receptor
体内研究

Eprotirome is a liver-selective thyroid hormone receptor agonist. Histological analysis of livers from mice treated with Eprotirome reveals that Eprotirome elicits a near complete elimination of lipid filled vacuoles that are characteristic of the livers from untreated control mice. Eprotirome treated mice also exhibit increased fasting glucose, but Eprotirome does not increase fasting insulin levels. Glucose levels of mice treated with Eprotirome continues to increase over time, leading to pronounced hyperglycemia by the end of the study. Temperature of mice treated with Eprotirome is decreased relative to untreated control mice.

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