Eprotirome (KB2115)
(Synonyms: 伊罗替罗,KB2115) 目录号 : GC33764
A thyroid hormone mimetic
Cas No.:355129-15-6
Sample solution is provided at 25 µL, 10mM.
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The thyroid hormones, thyroxine (T4) and triiodothyronine (T3), promote the reduction of plasma cholesterol levels and induce weight loss. However when administered in high doses, thyroid hormones produce undesirable side effects in the heart, bone and muscle. KB2115 is a synthetic thyroid hormone mimetic. At a dose of 50-
1.Berkenstam, A., Kristensen, J., Mellstr?m, K., et al.The thyroid hormone mimetic compound KB2115 lowers plasma LDL cholesterol and stimulates bile acid synthesis without cardiac effects in humansProc. Natl. Acad. Sci. USA105(2)663-667(2008)
Animal experiment: | Twelve-week old male ob/ob mice are used in this study. A catheter is implanted into the right internal jugular vein before the hyperinsulinemic-euglycemic clamp. After recovery, mice are administered Eprotirome (0.3 mg/kg) via intraperitoneal injection for 10 days. On the day of the clamp experiment, conscious, overnight-fasted mice receive a primed (10 μCi) and constant rate intravenous infusion (0.1 μCi /min) of [3-3H] glucose to measure basal glucose turnover. After 60 to 75 minutes of labeled glucose infusion, the hyperinsulinemic-euglycemic clamp is performed with continuous infusion of insulin (12 mU/kg/min) and variable infusion of 25% glucose to maintain euglycemia (~120 mg/dL). Blood samples are collected by tail bleeding (approximately every 10 min) to measure blood glucose concentrations[1]. |
References: [1]. 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):e0122987. | |
| Cas No. | 355129-15-6 | SDF | |
| 别名 | 伊罗替罗,KB2115 | ||
| Canonical SMILES | O=C(O)CC(NC1=CC(Br)=C(OC2=CC=C(O)C(C(C)C)=C2)C(Br)=C1)=O | ||
| 分子式 | C18H17Br2NO5 | 分子量 | 487.14 |
| 溶解度 | DMSO : 125 mg/mL (256.60 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.0528 mL | 10.264 mL | 20.528 mL |
| 5 mM | 0.4106 mL | 2.0528 mL | 4.1056 mL |
| 10 mM | 0.2053 mL | 1.0264 mL | 2.0528 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet