Bioactivity | 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]. |
Target | IC50: 0.03 μM (THR-β) and 0.22 μM (THR-α) |
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]. |
Name | THR-β agonist 6 |
CAS | 2791290-58-7 |
Formula | C20H14Cl2N6O3 |
Molar Mass | 457.27 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [1]. Liuyu Hu, et al. Discovery of Highly Potent and Selective Thyroid Hormone Receptor β Agonists for the Treatment of Nonalcoholic Steatohepatitis. J Med Chem. 2023 Mar 9;66(5):3284-3300. |