Eprotirome 是一种肝脏选择性甲状腺激素受体 (thyroid hormone receptor, TR) 激动剂。它对TRβ的亲和力略高于TRα。它降低了低密度脂蛋白 (LDL) 胆固醇的浓度，可用于研究血脂异常和肥胖症。

Eprotirome, a synthetic thyroid hormone mimetic, is a thyroid hormone receptor agonist.

In moderately overweight and hypercholesterolemic subjects Eprotirome (KB2115) was found to be safe and well tolerated and elicited up to a 40% lowering of total and LDL cholesterol after 14 days of treatment. Bile acid synthesis was stimulated without evidence of increased cholesterol production [1]. KB2115 treated mice exhibited increased fasting glucose, although KB2115 did not increase fasting insulin levels [2].

A catheter was implanted into the right internal jugular vein before the hyperinsulinemic-euglycemic clamp. After recovery, mice were administered GC-1 (0.03 or 0.3 mg/kg), KB2115 (0.3 mg/kg) or T3 (0.06 mg/kg) via intraperitoneal injection for 10 days. On the day of the clamp experiment, conscious, overnight-fasted mice received a primed (10 μCi) and constant rate intravenous infusion (0.1 uCi/min) of [3-3H] glucose to measure basal glucose turnover. After 60–75 minutes of labeled glucose infusion, the hyperinsulinemic-euglycemic clamp was performed with continuous infusion of insulin (12 mU/kg/min) and variable infusion of 25% glucose to maintain euglycemia (~120 mg/dl). Blood samples were collected by tail bleeding (approximately every 10 min) to measure blood glucose concentrations [2].

355129-15-6

C18H17Br2NO5

487.144

伊罗替罗;KB2115

Ethanol:30 mg/mL
DMSO:90 mg/mL (184.75 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years