| Bioactivity | F44-A13 is an orally active and highly selective farnesoid X receptor (FXR) antagonist with an IC50 value of 1.1 μM. F44-A13 can optimize cholesterol metabolism and reduce its activity by inducing CYP7A1 expression. F44-A13 reduces levels of cholesterol, triglycerides, and low-density lipoprotein cholesterol (LDL-C) in mouse models. F44-A13 can be used in the study of metabolic diseases associated with lipid disorders[1]. |
| Invitro | F44-A13 对多种核受体具有高度选择性，包括视黄酸受体 α/β/γ (RARα/β/γ)，视黄酮 X 受体 α/β/γ，(RXRα/β/γ)，孕烷 X 受体 (PXR)，过氧化物酶体增殖激活受体 α/β (PPARα/β)，甲状腺激素受体 β (THRβ)，以及与视黄酸受体相关的孤儿受体 γ (RORγ)[1]。F44-A13 (50 μM, 24 小时) 在 50 μM CDCA (HY-76847) 的存在下，以剂量依赖性方式抑制 FXR 的转录活性，IC50 值为 3.0 μM，F44-A13 为低毒性、高选择性的 FXR 拮抗剂[1]。F44-A13 (F44-A13: 3, 10, 30 μM; CDCA: 100 μM; 24 小时) 能通过诱导 CYP7A1 的表达改善胆固醇代谢，降低胆固醇的活性。F44-A13 能使 Shp 和 Bsep 的表达水平降低，CYP7A1 的表达水平升高[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> F44-A13 相关抗体: Cell Viability Assay[1] Cell Line: |
| In Vivo | F44-A13 (20, 40 mg/kg; 口服和腹腔注射; 4 天) 在 C57BL/6 mice 小鼠模型中能有效地降低总胆固醇 (TC)，甘油三酯 (TG) 和低密度脂蛋白胆固醇 (LDL-C) 的水平[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: |
| CAS | 1338190-14-9 |
| Formula | C28H40N4O5S |
| Molar Mass | 544.71 |
| 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]. Dou X, et al. Discovery of novel and selective farnesoid X receptor antagonists through structure-based virtual screening, preliminary structure-activity relationship study, and biological evaluation. Eur J Med Chem. 2024;269:116323. |