2. Vitamin D Related/Nuclear Receptor
  3. Thyroid Hormone Receptor
  4. THR-β agonist 6

THR-β agonist 6 是一种具有口服活性的，选择性甲状腺激素受体 β (THR-β) 激动剂，对 THR-β 和 THR-α 的 EC50 分别为 0.03 μM 和 0.22 μM。THR-β agonist 6 在小鼠中表现出 93:1 的出色肝血清比。THR-β agonist 6 具有用于非酒精性脂肪性肝炎 (NASH) 研究的潜力。

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THR-β agonist 6 Chemical Structure

THR-β agonist 6 Chemical Structure

CAS No. : 2791290-58-7

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THR-β agonist 6 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

THR-β agonist 6 is an orally active, selective thyroid hormone receptor β (THR-β) agonist with EC50s of 0.03 μM and 0.22 μM for THR-β and THR-α, respectively. THR-β agonist 6 exhibits an xcellent liver-to-serum ratio of 93:1 in mice. THR-β agonist 6 has the potential for nonalcoholic steatohepatitis (NASH) research[1].

IC50 & Target

IC50: 0.03 μM (THR-β) and 0.22 μM (THR-α)[1]
体内研究
(In Vivo)

THR-β agonist 6 (3, 10 mg/kg; 口服灌胃; 每天一次; 持续 6 周) 剂量依赖性显着降低 HFD-CCl4 诱导的血清总胆固醇和低密度脂蛋白-胆固醇水平[1]。
THR-β agonist 6 (3, 10 mg/kg; 口服灌胃; 单次剂量) 对 ICR 小鼠在 10 和 3 mg/kg 时显示 TC 减少超过 30%，并有效地将血清 LDL-C (LDL-胆固醇) 水平降低 62.1% 和 53.6% kg[1]。
THR-β agonist 6 (3, 10 mg/kg; 口服灌胃; 单次剂量) 显着上调 Dio1、Thrsp 和 Me1 mRNA 水平 19、16 和 3 倍以上[1]。
Pharmacokinetic Parameters of THR-β agonist 6 in mice[1].

PO (30 mg/kg)
Tmax (h) 8.7
Cmax (ng/mL) 2830
AUClast (h*ng/mL) 37536
t1/2 (h) 8.7

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male C57BL/6J mice (4-5 weeks) fed a high-fat diet (HFD) for 10 weeks[1]
Dosage: 3, 10 mg/kg
Administration: Orally; once daily for 6 weeks
Result: Prominently reduced HFD-CCl4-induced (CCl4; ip; 0.05 mL/kg) serum total cholesterol and LDL-cholesterol levels in a dose-dependent manner.
Markedly reduced the liver steatosis and inflammation score.
分子量

457.27

Formula

C20H14Cl2N6O3
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

THR-β agonist 6 相关分类

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

THR-β agonist 62791290-58-7Thyroid Hormone ReceptorTHROrallythyroid hormone receptor βTHR-βTHR-αliver-to-serum rationonalcoholic steatohepatitisNASHInhibitorinhibitorinhibit

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产品名称：
THR-β agonist 6
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