2. Vitamin D Related/Nuclear Receptor PI3K/Akt/mTOR Epigenetics Metabolic Enzyme/Protease
  3. Thyroid Hormone Receptor AMPK Acetyl-CoA Carboxylase Mitochondrial Metabolism
  4. THR-β agonist 9

THR-β agonist 9 是一种强效、选择性且对 His435 突变敏感的 THR-β 激动剂 (EC50：3.2 nM)。THR-β agonist 9 具有中等选择性 (约 10 倍) 和良好的多种 His435 突变体 (H435A, H435Y, and H435R) 活化能力 (EC50：134.2 nM 至 515.5 nM)。THR-β agonist 9 具有研究血脂异常、代谢功能障碍相关脂肪性肝炎 (MASH) 或甲状腺激素耐药性 (RTH) 的潜力。

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THR-β agonist 9 Chemical Structure

THR-β agonist 9 Chemical Structure

CAS No. : 2920045-74-3

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THR-β agonist 9 相关抗体

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NUAK1 NUAK2 AMPK AMPK α1β1γ1 AMPK α2β1γ1 AMPK α1β2γ1 AMPK α2β2γ1

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

THR-β agonist 9 is a potent, selective, and His435 mutation-sensitive THR-β (EC50: 3.2 nM) agonist. THR-β agonist 9 has moderate selectivity (approximately 10-fold) and good activation capacity (EC50: 134.2 nM to 515.5 nM) for multiple His435 mutants (H435A, H435Y, and H435R). THR-β agonist 9 has the potential to be used in the study of dyslipidemia, metabolic dysfunction-associated steatohepatitis (MASH), or resistance to thyroid hormone (RTH)[1].

IC50 & Target

THR-β with an EC50 of 258.2 nM
体外研究
(In Vitro)

THR-β agonist 9 (Compound 15n) ( 1 μM) 可激活 THR-β，EC50 为 258.2 nM，对 THR-α 的激活效价为 1707.0 nM，在基于细胞的报告基因检测中表现出优异的选择性[1]。

THR-β agonist 9 同时激活三种突变体，EC50分别为 THR-βH435A (515.5 nM)、THR-βH435R (134.2 nM) 和 THR-βH435Y (513.1 nM)[1]。

THR-β agonist 9 (1-10 μM，24 小时) 可降低小鼠原代肝细胞和 HepG2 细胞中的 TG 和 TC 水平，减少脂质蓄积[1]。

THR-β agonist 9 (1-10 μM，24 小时) 增加了 HepG2 细胞的基础和未偶联线粒体呼吸[1]。

THR-β agonist 9 (1-10 μM，24 小时)增加 AMPK 和 ACC 的磷酸化，并伴有更高的 CPT1 蛋白水平，通过 AMPK 通路改善 HepG2 细胞的代谢[1]。

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

THR-β agonist 9 相关抗体:

Western Blot Analysissup>[1]

Cell Line: HepG2 cells
Concentration: 1 μM, 3 μM, 10 μM
Incubation Time:
Result: Increased phosphorylation of AMPK and ACC, accompanied by higher protein levels of CPT1.

Cell Cytotoxicity Assaysup>[1]

Cell Line: THR-β-positive cells (HepG2 and primary mouse liver cells) and a THRβ-negative cell lines (NCIH460, lung cancer)
Concentration: 10 μM
Incubation Time: 72 h
Result: Did not show cell proliferation inhibition activity in two THR-β-positive HepG2 cells and NCIH460.
分子量

418.40

Formula

C23H18N2O6
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 9 相关分类

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  • Do most proteins show cross-species activity?

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Keywords:

THR-β agonist 92920045-74-3Thyroid Hormone ReceptorAMPKAcetyl-CoA CarboxylaseMitochondrial MetabolismTHRAMP-activated protein kinaseACC, Acetyl Coenzyme A CarboxylaseAgonistDyslipidemiaMASHRTHHepG2 cellsPrimary mouse liver cellsInhibitorinhibitorinhibit

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