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CAS No.: 355129-15-6

Eprotirome Catalog No. CSN21329

Synonyms: KB2115;LEI-110: KB-2115

Eprotirome is a liver-selective thyroid hormone receptor agonist.

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400-920-2911

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生物活性

实验方案

技术信息

生物活性

描述Thyroid hormone is potential to mediate favorable effects on lipid metabolism and energy expenditure, decreasing plasma low-density lipoprotein (LDL) and increasing energy expenditure through futile substrate cycling and increasing thermogenesis. Thyroid hormones act primarily via three nuclear receptors, TRα1, TRβ1, and TRβ2^[1]. Eprotirome (KB2115) is a liver-selective thyroid hormone receptor agonist. In patients with hypercholesterolemia, the addition of placebo or eprotirome at a dose of 25, 50, or 100 mg daily to statin treatment for 12 weeks reduced the mean level of serum LDL cholesterol from 141 mg per deciliter (3.6 mM) to 127, 113, 99, and 94 mg per deciliter (3.3, 2.9, 2.6, and 2.4 mM), respectively, (mean reduction from baseline, 7%, 22%, 28%, and 32%)^[2]. In vivo, one-week treatment with IP injections of KB2115 (25 and 12.5 μg/100 g b.w.) induced a strong hepatocyte proliferation in F-344 male rats^[3].
临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT00677248	Hypercholesterolemia	Phase 2	Completed	-	Sweden ... more >> Karo Bio AB HUddinge, Sweden Collapse <<
NCT01410383	Heterozygous Familial Hypercho... more >>lesterolaemia Collapse <<	Phase 3	Terminated	October 2014	-
NCT00776321	Primary Hypercholesterolemia	Phase 2	Completed	-	Sweden ... more >> Jens Kristensen Huddinge, Sweden Collapse <<

参考文献

[1] Vatner DF, Weismann D, Beddow SA, et al. Thyroid hormone receptor-β agonists prevent hepatic steatosis in fat-fed rats but impair insulin sensitivity via discrete pathways. Am J Physiol Endocrinol Metab. 2013;305(1):E89-E100.
[2] Ladenson PW, Kristensen JD, Ridgway EC, et al. Use of the thyroid hormone analogue eprotirome in statin-treated dyslipidemia. N Engl J Med. 2010;362(10):906-916.
[3] Szydlowska M, Pibiri M, Perra A, et al. The Thyromimetic KB2115 (Eprotirome) Induces Rat Hepatocyte Proliferation. Gene Expr. 2017;17(3):207-218.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.0528 mL
- 10.2640 mL
- 20.5280 mL
- 5 mM
- 0.4106 mL
- 2.0528 mL
- 4.1056 mL
- 10 mM
- 0.2053 mL
- 1.0264 mL
- 2.0528 mL

技术信息

CAS号

355129-15-6

储存条件

粉末: Sealed in dry,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C18H17Br2NO5

运输

蓝冰

分子量

487.14

别名

KB2115;LEI-110: KB-2115

溶解度

DMSO	125.0 mg/mL (256.6 mM)
Water	insoluble

动物实验配方

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