PeptideDB

THR-β agonist 6

CAS: 2791290-58-7 F: C20H14Cl2N6O3 W: 457.27

THR-β agonist 6 is an orally active, selective thyroid hormone receptor β (THR-β) agonist with EC50s of 0.03 μM and
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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.