gal4

BMS-687453 是一种选择性 PPARα激动剂，对人 PPARα的 EC50和 IC50分别为 10 nM 和 260 nM。它较弱地抑制 PPARγ 的活性，EC50和 IC50值分别为 4100 nM 和大于 15000 nM。

PX20606 是一种口服生物活性的法呢醇 X 受体 (FXR) 激动剂，在 Gal4-FXR 测定中，其 EC50 为 220 nM (mFXR) 和 50 nM (hFXR)。PX20606 能诱导肿瘤抑制基因 NDRG2 的表达，并抑制小鼠肝细胞癌 (HCC) 模型中的肿瘤生长和转移，同时具备肝脏保护活性。

GW590735 is a potent and selective agonist of PPARα with an EC50 value of 4 nM for the expression a GAL4-responsive reporter gene and at least 500-fold selectivity versus PPARγ and PPARδ. GW590735 significantly increased HDL cholesterol, decreased LDL and VLDL cholesterol, and significantly reduced triglycerides. Maximal increases in HDL cholesterol were 37%, 53%, and 84% with fenofibrate, torcetrapib, and GW590735, respectively.

BMS-986318 是一种有效的非胆汁酸FXR 激动剂，在FXRGal4 和 SRC-1 募集试验中的EC50分别为 53 和 350 nM。 BMS-986318 具有合适的 ADME 特性，并在肝胆汁淤积和纤维化的小鼠胆管结扎模型中具有效果。BMS-986318 可用于非酒精性脂肪性肝炎 (NASH)的研究。

Atorvastatin ethyl ester, a derivative of Atorvastatin, exhibits potent inhibition of 9-cis-RA-induced Gal4 reporter activity.

Atorvastatin methyl ester is a derivative of Atorvastatin. It inhibits the 9-cis-RA-induced Gal4 reporter activity more strongly than Atorvastatin.

BMS-986251 is a potent and specific RORγt inverse agonist that exerts its action via oral administration. It shows an EC 50 of 12 nM for RORγt GAL4. In human whole blood assay, BMS-986251 effectively inhibits IL-17 with an EC 50 of 24 nM. Furthermore, BMS-986251 exhibits strong therapeutic effects in mouse acanthosis and Imiquimod-induced models, which are commonly used preclinical models for psoriasis.