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

Deoxycholic Acid (cholanoic acid)一种胆汁酸，是肠道代谢的副产物，激活G蛋白偶联胆汁酸受体TGR5。

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

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

Vonafexor is a farnesoid X receptor agonist.

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

GW4064 is a selective, non-steroidal farnesoid X receptor (FXR) agonist (EC50 = 15 nM).

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

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.

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.

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 .

25-Hydroxycholesterol is a potent and selective suppressor of IgA production by B cells wit EC50 about 65 nM.

Bufalin a major digoxin-like immunoreactive component of the Chinese medicine Chan Su and has been shown to exert a potential for anticancer activity against various human cancer cell lines in vitro.