| Name | Eprotirome |
| Description | Eprotirome (KB2115), a synthetic thyroid hormone mimetic, is a thyroid hormone receptor agonist. |
| Animal Research | 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]. |
| In vivo | 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]. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | Ethanol : 30 mg/mL (61.58 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 3.3 mg/mL (6.77 mM), Sonication is recommended.
DMSO : 90 mg/mL (184.75 mM), Sonication is recommended.
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| Keywords | Thyroidhormonereceptor(THR) | Thyroidhormonereceptor | Thyroid hormone receptor(THR) | Thyroid hormone receptor | THR | KB-2115 | KB 2115 | Inhibitor | inhibit | Eprotirome |
| Inhibitors Related | Azetirelin | L-Thyroxine sodium | Resmetirom | 2,2-BIS(2-HYDROXY-5-BIPHENYLYL)PROPANE | Iopanoic acid | DS08210767 | Carbimazole | Octinoxate | Methimazole | PCO371 | Tiratricol | Eneboparatide |
| Related Compound Libraries | Nuclear Receptor Compound Library | Failed Clinical Trials Compound Library | Target-Focused Phenotypic Screening Library | Bioactive Compound Library | ReFRAME Related Library | Anti-Obesity Compound Library | Drug Repurposing Compound Library | Endocrinology-Hormone Compound Library | NO PAINS Compound Library | Clinical Compound Library | Bioactive Compounds Library Max | Anti-Metabolism Disease Compound Library |
United States
