产品说明书
Eprotirome
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同义名 : | KB2115 |
| CAS号 : | 355129-15-6 | |
| 货号 : | A597483 | |
| 分子式 : | C18H17Br2NO5 | |
| 纯度 : | 99%+ | |
| 分子量 : | 487.139 | |
| MDL号 : | MFCD11045847 | |
| 存储条件： |
粉末 Sealed in dry,Room Temperature 液体 -20°C:3-6个月-80°C:12个月 |
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| 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 |
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| 动物实验配方： |
| 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 ... 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 << |
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.05mL 0.41mL 0.21mL |
10.26mL 2.05mL 1.03mL |
20.53mL 4.11mL 2.05mL |
| 参考文献 |
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