| 产品描述: | Eprotirome, a synthetic thyroid hormone mimetic, is a thyroid hormone receptor agonist. |
| 靶点: |
Thyroid hormone receptor(THR);Thyroidhormonereceptor(THR) |
| 体内研究: |
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 |
| 动物实验: |
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 |
| 参考文献: |
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. |
| 溶解性: |
Soluble in DMSO、Ethanol |
| 保存条件: |
2-8℃ |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
2.053 ml |
10.264 ml |
20.528 ml |
| 5 mM |
0.411 ml |
2.053 ml |
4.106 ml |
| 10 mM |
0.205 ml |
1.026 ml |
2.053 ml |
| 50 mM |
0.041 ml |
0.205 ml |
0.411 ml |
|
| 注意: |
部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。 |