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Endocrinology/Hormones Thyroid hormone receptor(THR) Eprotirome

Eprotirome

Catalog No. T5360   CAS 355129-15-6
Synonyms: KB2115, KB2115

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

Eprotirome, CAS 355129-15-6
Pack Size Availability Price/USD Quantity
1 mg In Stock 182.00
5 mg In Stock 284.00
10 mg In Stock 393.00
25 mg In Stock 638.00
50 mg In Stock 940.00
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Eprotirome, a synthetic thyroid hormone mimetic, is a thyroid hormone receptor agonist.
Targets&IC50 THR,  
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].
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].
Synonyms KB2115 , KB2115
Purity 98.25%
Molecular Weight 487.14
Formula C18H17Br2NO5
CAS No. 355129-15-6

Storage

0-4℃ for short term (days to weeks), or -20℃ for long term (months).

Solubility Information

DMSO: 90 mg/mL (184.75 mM)

Ethanol: 30 mg/mL

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Citations

References and Literature
1. Berkenstam A, et al. The thyroid hormone mimetic compound KB2115 lowers plasma LDL cholesterol and stimulates bile acid synthesis without cardiac effects in humans. Proc Natl Acad Sci U S A. 2008 Jan 15;105(2):663-7. 2. Martagón AJ, et al. The amelioration of hepatic steatosis by thyroid hormone receptor agonists is insufficient to restore insulin sensitivity in ob/ob mice. PLoS One. 2015 Apr 7;10(4):e201221987.

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