1. Vitamin D Related/Nuclear Receptor
  2. Thyroid Hormone Receptor
  3. THR-β agonist 11

THR-β agonist 11 是一种口服活性且选择性的甲状腺激素受体 (THR-β) 激动剂。THR-β agonist 11 在喂食胆固醇的大鼠中显示出强效的降胆固醇活性。THR-β agonist 11 显著降低高脂饮食-四氯化碳 (HFD-CCl4) 诱导的代谢功能障碍相关脂肪性肝炎 (MASH) 模型小鼠的血清总甘油三酯 (TG)、低密度脂蛋白胆固醇 (LDL-cholesterol)、肝脏总胆固醇 (TC) 和 TG 水平,并缓解肝脂肪变性、炎症和纤维化。THR-β agonist 11 可用于代谢功能障碍相关脂肪性肝炎 (MASH) 及其他纤维化疾病的研究。

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THR-β agonist 11

THR-β agonist 11 Chemical Structure

CAS No. : 3051970-23-8

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  • 生物活性

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  • 参考文献

生物活性

THR-β agonist 11 is an orally active and selective thyroid hormone receptor (THR-β) agonist. THR-β agonist 11 shows potent cholesterol-lowering activity in cholesterol-fed rats. THR-β agonist 11 significantly reduces serum total TG, LDL-cholesterol, liver total TC and TG levels, and alleviates hepatic steatosis, inflammation and fibrosis in HFD-CCl4-induced Metabolic dysfunction-associated steatohepatitis (MASH) model mice. THR-β agonist 11 can be used for the study of metabolic dysfunction-associated steatohepatitis (MASH) and other fibrotic diseases[1].

体内研究
(In Vivo)

THR-β agonist 11 (Compound 29a) (0.5 mg/kg,口服,单次给药,24 小时) 在喂食胆固醇的 Sprague-Dawley 大鼠中表现出优越的降胆固醇效果[1]
THR-β agonist 11 (3 mg/kg,口服,每日一次,持续 6 周) 显著降低高脂饮食-四氯化碳 (HFD-CCl4) 诱导的 MASH 模型 C57BL/6J 小鼠的血清总甘油三酯 (TG)、低密度脂蛋白胆固醇 (LDL-cholesterol)、肝脏总胆固醇 (TC) 和 TG 水平[1]

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

Animal Model: Male Sprague-Dawley rats were fed a normal chow diet supplemented with 1.5% cholesterol and 0.5% cholic acid (w/w) for 2 weeks to establish the model[1]
Dosage: 0.5 mg/kg
Administration: p.o., single administration, 24 h
Result: Achieved a total plasma cholesterol reduction rate of 29.07%.
Animal Model: 4-week-old male C57BL/6J mice were fed a high-fat diet (HFD) for 10 weeks to induce obesity, then intraperitoneally injected with carbon tetrachloride (CCl4) twice a week for 6 weeks to establish the MASH model[1]
Dosage: 3 mg/kg
Administration: p.o., once daily, 6 weeks
Result: Reduced serum total TG, LDL-cholesterol, liver total TC and TG levels.
Decreased serum ALT and AST levels by a notable margin.
Alleviated hepatic steatosis, inflammation and fibrosis.
Downregulated the mRNA expression levels of fibrosis markers Tgfb1 and Acta2.
分子量

516.95

Formula

C26H30ClN2O5P

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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  • 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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THR-β agonist 11
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HY-178015
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