1. Vitamin D Related/Nuclear Receptor
  2. Thyroid Hormone Receptor
  3. TRβ agonist-4

TRβ agonist-4 是一种具有生物口服利用度、肝脏靶向性的 hTHR-β 选择性激动剂 (EC50=6.0nM),对 THR-α 的选择性达 105.3 倍。TRβ agonist-4 同时存在多种晶型,包括晶型 A、B、C、D、E 以及无定形形式。TRβ agonist-4 可用于非酒精性脂肪性肝炎 (NASH) 的相关研究。

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TRβ agonist-4

TRβ agonist-4 Chemical Structure

CAS No. : 3066979-01-6

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

TRβ agonist-4 is an orally bioavailable, liver-targeted selective agonist of hTHR-β (EC50=6.0 nM), with a 105.3-fold selectivity over THR-α. TRβ agonist-4 exists in multiple crystal forms, including Form A, Form B, Form C, Form D, Form E, as well as an amorphous form. TRβ agonist-4 can be used for research related to non-alcoholic steatohepatitis (NASH)[1].

体外研究
(In Vitro)

TR-β agonist-4 (Compound 1) 的外消旋体,其 THR-β 激活活性在过表达肝特异性转运蛋白 SLCO1B1 的 HEK293T 细胞中显著增强,24 h 的 EC50 低至 13.4 nM,肝靶向性倍数达 24.9 (优于 MGL-3196 (HY-12216))[1]

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

体内研究
(In Vivo)

TR-β agonist-4 (Compound 1) 的外消旋体 (5 mg/kg) 可剂量依赖性地降低高脂饮食诱导的高脂血症小鼠的血清总胆固醇和低密度脂蛋白胆固醇水平[1]
TR-β agonist-4 (Compound 1) 的外消旋体 (0.5 mg/kg) 可显著降低 HFD+CCl4 诱导的非酒精性脂肪性肝炎小鼠的肝脏 TG、TC 水平及 NASH 评分,其疗效与 10 mg/kg MGL-3196 (HY-12216) 相当[1]

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

分子量

468.43

Formula

C23H19F3N6O2

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
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  • 稀释计算器

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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.

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TRβ agonist-4
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HY-182769
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