2. Vitamin D Related/Nuclear Receptor
  3. Thyroid Hormone Receptor
  4. THR-β agonist 10

THR-β agonist 10 是一种口服活性且选择性的 THR-β 激动剂，EC50 为 11 nM。THR-β agonist 10 可显著降低 ALT (丙氨酸氨基转移酶)、TC (总胆固醇)、LDL-C (低密度脂蛋白胆固醇) 水平，并在代谢功能障碍相关性脂肪性肝炎 (MASH) 小鼠模型中改善脂肪变性、气球样变、炎症和纤维化。THR-β agonist 10 可用于代谢功能障碍相关性脂肪性肝炎 (MASH) 的研究。

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THR-β agonist 10

THR-β agonist 10 Chemical Structure

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THR-β agonist 10 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 10 is an orally active and selective THR-β agonist, with an EC50 of 11 nM. THR-β agonist 10 significantly reduces ALT (Alanine Aminotransferase), TC (Total Cholesterol), and LDL-C (Low-Density Lipoprotein Cholesterol) levels, and improves steatosis, ballooning, inflammation and fibrosis in the metabolic dysfunction-associated steatohepatitis (MASH) mouse model. THR-β agonist 10 can be used for the study of MASH[1].

IC50 & Target[1]

THR-β

11 nM (EC50)

体外研究
(In Vitro)

THR-β agonist 10 (Compound 12) (16 h) 对 THR-β 表现出强效激动活性，EC50 为 11.0 nM[1]。
THR-β agonist 10 (0-100 μM，24 h) 在原代小鼠肝细胞和原代大鼠肝细胞中未表现出明显细胞毒性[1]。
THR-β agonist 10 对 CYP2C9 表现出弱抑制作用 (IC50 = 9.4 μM)，但对其他 CYP 酶 (CYP1A2、2C19、2D6、3A4-M、3A4-T) 无抑制作用，且 IC50 > 25 μM[1]。

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

THR-β agonist 10 相关抗体:
体内研究
(In Vivo)

THR-β agonist 10 (Compound 12) (3 mg/kg，口服，单次给药) 可显著降低小鼠血清总胆固醇和低密度脂蛋白胆固醇[1]。
THR-β agonist 10 (1-3 mg/kg，口服，每日一次，6 周) 可显著降低代谢障碍相关性脂肪性肝炎 (MASH) 小鼠的血清丙氨酸氨基转移酶、总胆固醇和低密度脂蛋白胆固醇水平[1]。

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

Animal Model: 7-8 week-old male ICR mice[1]
Dosage: 3 mg/kg
Administration: p.o., single dose
Result: Reduced serum total cholesterol by 34.2% and low-density lipoprotein cholesterol by 56.3%.
Animal Model: Male C57BL/6J mice (for MASH model): 4-5 week-old male C57BL/6J mice were first fed a high-fat diet for 14 weeks to induce obesity, then received intraperitoneal injections of Carbon tetrachloride (HY-Y0298) twice a week for an additional 6 weeks to establish the MASH model[1]
Dosage: 1 mg/kg or 3 mg/kg
Administration: p.o., once daily, 6 weeks
Result: Achieved significant decreases in serum alanine aminotransferase, total cholesterol, and low-density lipoprotein cholesterol levels.
Achieved reductions in NAFLD Activity Score (NAS) by improving steatosis, ballooning, and inflammation.
Showed effective alleviation of liver fibrosis.
分子量

530.32

Formula

C25H13Cl2N7O3
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 10 相关分类

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Help & FAQs
  • 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 10Thyroid Hormone ReceptorTHRmetabolic dysfunction-associated steatohepatitisALT (Alanine Aminotransferase)TC (Total Cholesterol)LDL-C (Low-Density Lipoprotein Cholesterol)THR-βInhibitorinhibitorinhibit

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