GW 4064 是一种 FXR 激动剂，IC50 值为 190 nM。GW 4064 具有调节胆固醇和脂质代谢的作用，主要用于研究代谢性疾病和肝脏疾病。

Fexaramine is a small molecule farnesoid X receptor (FXR) agonist with 100-fold increased affinity relative to natural compounds.

T0901317 is a selective agonist for LXR and FXR with EC50 of 50 nM and 5 μM, respectively.

WAY-362450 is an agonist of farnesoid X receptor (FXR) with EC50 of 4 nM. WAY-362450 is used to the treatment of dyslipidemia.

Tropifexor is a potent agonist of FXR with EC50 of 0.26 nM.

Cilofexor (GS-9674) 是一种有效的，选择性的，口服活性的非甾体 FXR 激动剂，EC50 为 43 nM。。在一项为期 12 周的研究中，Cilofexor 在原发性硬化性胆管炎患者中耐受良好，并显著改善了肝生化指标和胆汁淤积标志物。

DY268是一种法尼样 X 受体 (FXR) 的高效拮抗剂，在 time-resolved FRET 分析中，IC₅₀ 为 7.5 nM，抑制 FXR 反式激活的 IC₅₀ 为 468 nM，适用于代谢性疾病的相关研究。

Nidufexor is a potent farnesoid X receptor (FXR) agonist for the treatment of non-alcoholic steatohepatitis (NASH) and hepatobiliary disorders.

Obeticholic acid is a selective FXR agonist with EC50 of 99 nM and it has anticholestatic activity.

Vonafexor is a farnesoid X receptor agonist.

LY2562175 是一种高效且选择性的 FXR 激动剂，其 EC50 值为 193 nM。

(Z)-Guggulsterone is a broad spectrum steroid receptor ligand and an antagonist of FXR with antiseptic, antirheumatic and anti-inflammatory activity in vivo.

Guggulsterone is a plant sterol derived from the gum resin of the tree Commiphora wightii. Guggulsterone inhibits the growth of a wide variety of tumor cells and induces apoptosis through down regulation of antiapoptotic gene products (IAP1, xIAP, Bfl-1/A1, Bcl-2, cFLIP and survivin), modulation of cell cycle proteins (cyclin D1 and c-Myc), activation of caspases and JNK, inhibition of Akt. Guggulsterone, a farnesoid X receptor (FXR) antagonist, decreases CDCA-induced FXR activation with IC50s of 17 and 15 μM for Z- and E-Guggulsterone, respectively.

Morroniside is a naturally occuring iridoid which can regulate hair growth and cycle transition via activation of the Wnt/β-catenin signaling pathway.

Gracillin is a kind of steroidal saponin isolated and purified from the roots of Dioscorea opposita Thunb. and the root bark of wild yam Dioscorea nipponica with antitumor agent.

Madecassic acid, a natural product isolated and purified from the herbs of Centella asiatica (L.) Urban, has anti-inflammatory properties by iNOS, COX-2, TNF-alpha, IL-1beta, and IL-6 inhibition via the downregulation of NF-kappaB activation in RAW 264.7 macrophage cells.

Periplocin is a cardiotonic steroid isolated from Periploca forrestii. Periplocin promotes tumor cell apoptosis and inhibits tumor growth. Periplocin has the potential to facilitate wound healing through the activation of Src/ERK and PI3K/Akt pathways mediated by Na/K-ATPase .

Cyasterone is an inhibitor of EGFR that maybe a promising anti-cancer agent espcially in skin carcinoma.

Fucosterol是一种从藻类、海藻或硅藻中分离出的甾醇，具有抗氧化、抗脂肪、降胆固醇、抗糖尿病和抗癌等多种生物活性，通过抑制 PPARα 和 C/EBPα 的表达调控脂肪生成，可用于抗肥胖药物的开发研究。

Diosgenin glucoside is a natural product isolated and purified from the roots of Trillium tschonoskii Maxim., which may be of use in the management of hypercholesterolemia and atherosclerosis.