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Eprotirome {[allProObj[0].p_purity_real_show]}

货号:A597483 同义名: KB2115

Eprotirome is a liver-selective thyroid hormone receptor agonist.

Eprotirome 化学结构 CAS号:355129-15-6
Eprotirome 化学结构
CAS号:355129-15-6
Eprotirome 3D分子结构
CAS号:355129-15-6
Eprotirome 化学结构 CAS号:355129-15-6
Eprotirome 3D分子结构 CAS号:355129-15-6
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Eprotirome 纯度/质量文件 产品仅供科研

货号:A597483 标准纯度: {[allProObj[0].p_purity_real_show]}
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Eprotirome 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].

Eprotirome 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 ... 展开 >> Karo Bio AB HUddinge, Sweden 收起 <<
NCT01410383 Heterozygous Familial Hypercho... 展开 >>lesterolaemia 收起 << Phase 3 Terminated October 2014 -
NCT00776321 Primary Hypercholesterolemia Phase 2 Completed - Sweden ... 展开 >> Jens Kristensen Huddinge, Sweden 收起 <<

Eprotirome 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.

Eprotirome 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.05mL

0.41mL

0.21mL

10.26mL

2.05mL

1.03mL

20.53mL

4.11mL

2.05mL

Eprotirome 技术信息

CAS号355129-15-6
分子式C18H17Br2NO5
分子量 487.139
别名 KB2115
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,Room Temperature

溶解度

DMSO: 120 mg/mL(246.34 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方
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