355129-15-6
中文名稱
伊羅替羅
英文名稱
Eprotirome
CAS
355129-15-6
分子式
C18H17Br2NO5
分子量
487.14
MOL 文件
355129-15-6.mol
更新日期
2023/03/20 15:41:19
355129-15-6 結(jié)構(gòu)式
基本信息
中文別名
伊羅替羅N-[3,5-二溴-4-(4-羥基-3-異丙基苯氧基)苯基]丙酰胺酸
3-((3,5-二溴-4-(4-羥基-3-異丙基苯氧基)苯基)氨基)-3-氧丙酸
英文別名
Kb-2115eprotirome
Unii-958aq7B6R1
KB2115 Exclusive
VPCSYAVXDAUHLT-UHFFFAOYSA-N
N-[3,5-Dibromo-4-(4-hydroxy-3-isopropylphenoxy)phenyl]malonamic acid
3-((3,5-Dibromo-4-(4-hydroxy-3-(1-methylethyl)phenoxy)phenyl)amino)-3-oxopropanoic acid
Propanoic acid,3-[[3,5-dibroMo-4-[4-hydroxy-3-(1-Methylethyl)phenoxy]phenyl]aMino]-3-oxo-
物理化學(xué)性質(zhì)
沸點(diǎn)596.3±50.0 °C(Predicted)
密度1.708
儲(chǔ)存條件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)
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)
酸度系數(shù)(pKa)3.16±0.32(Predicted)
形態(tài)A crystalline solid
顏色White to light yellow
常見問題列表
生物活性
Eprotirome (KB2115) 是肝臟選擇性甲狀腺激素受體 (thyroid hormone receptor, TR) 激動(dòng)劑。KB2115 對(duì) TRβ 的親和力略高于 TRα。Eprotirome 降低了低密度脂蛋白 (LDL) 膽固醇的濃度，可用于血脂異常和肥胖癥的研究。靶點(diǎn)
Thyroid hormone receptor
體內(nèi)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.