Eprotirome

SKU: orb1301854

Description

Eprotirome (KB2115) is a synthetic agonist of the thyroid hormone receptor. It serves as a research tool for studying lipid metabolism and has been investigated in preclinical in vivo models for potential applications in treating hypercholesterolemia.

Research Area

Metabolism Research

Key Properties

• CAS Number: 355129-15-6
• MW: 487.14
• Purity: 98.56% (May vary between batches)
• Formula: C₁₈H₁₇Br₂NO₅
• SMILES: CC(C)c1cc(Oc2c(Br)cc(NC(=O)CC(O)=O)cc2Br)ccc1O
• Target: Thyroid hormone receptor(THR)
• Solubility: Ethanol:30 mg/mL (61.58 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:3.3 mg/mL (6.77 mM);DMSO:90 mg/mL (184.75 mM)

Bioactivity

• 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 . KB2115 treated mice exhibited increased fasting glucose, although KB2115 did not increase fasting insulin levels .
• 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 .

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

inhibit, KB2115, KB-2115, KB 2115, Eprotirome, Inhibitor, THR, Thyroid Hormone Receptor, Thyroid hormone receptor, Thyroid hormone receptor(THR), Thyroidhormonereceptor, Thyroidhormonereceptor(THR)

Compound Identifiers

PubChem CID

10299876