2791290-58-7
2791290-58-7 structure
- Name: THR-β agonist 6
- Chemical Name: THR-β agonist 6
- CAS Number: 2791290-58-7
- Molecular Formula: C20H14Cl2N6O3
- Molecular Weight: 457.27
- Catalog: Research Areas Inflammation/Immunology
- Create Date: 2023-06-13 18:19:43
- Modify Date: 2024-01-05 09:45:17
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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].
| Name | THR-β agonist 6 |
|---|
| Description | 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]. |
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| Related Catalog | |
| Target |
IC50: 0.03 μM (THR-β) and 0.22 μM (THR-α)[1] |
| 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]. PO (30 mg/kg) Tmax (h) 8.7 Cmax (ng/mL) 2830 AUClast (h*ng/mL) 37536 t1/2 (h) 8.7 Animal Model: Male C57BL/6J mice (4-5 weeks) fed a high-fat diet (HFD) for 10 weeks[1] Dosage: 3, 10 mg/kg Administration: Orally; once daily for 6 weeks Result: Prominently reduced HFD-CCl4-induced (CCl4; ip; 0.05 mL/kg) serum total cholesterol and LDL-cholesterol levels in a dose-dependent manner. Markedly reduced the liver steatosis and inflammation score. |
| References |
| Molecular Formula | C20H14Cl2N6O3 |
|---|---|
| Molecular Weight | 457.27 |