Eprotirome (KB2115)

目录号: GC33764纯度: >99.50%同义词: 伊罗替罗,KB2115
A thyroid hormone mimetic

Eprotirome (KB2115)
Cas No.: 355129-15-6
规格价格库存数量操作
1mg¥148.00现货
1
5mg¥336.00现货
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10mg¥532.00现货
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25mg¥1,067.00现货
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50mg¥1,677.00现货
1
100mg¥2,689.00现货
1
10mM (in 1mL DMSO)¥360.00现货
1

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产品描述 Description

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 50-200 ?g administered to humans once-daily for 14 days, KB2115 lowers total and low-density lipoprotein cholesterol up to 40% without affecting high-density lipoprotein cholesterol levels and without deleterious side effects to the cardiovascular system.1 Unlike the statin class of drugs which decrease cholesterol synthesis, KB2115 stimulates cholesterol catabolism to bile acids without affecting cholesterol synthesis.1

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)

实验参考方法 Experimental Reference Method

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.

产品文档 Product Documents

Purity:>99.50%

化学性质Chemical Properties

CAS 号
355129-15-6
同义词
伊罗替罗,KB2115
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 g/mol
溶解性
DMSO : 125 mg/mL (256.60 mM)
保存条件
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°C,然后在超声波浴中震荡一段时间。
Shipping Condition
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