SBI-115

SBI-115
Identifiers
	IUPAC name (3-methylphenyl) 5-chloro-2-ethylsulfonylpyrimidine-4-carboxylate;
CAS Number	882366-16-7;
PubChem CID	18879973;
ChemSpider	11981745;
Chemical and physical data
Formula	C14H13ClN2O4S
Molar mass	340.78 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES CCS(=O)(=O)C1=NC=C(C(=N1)C(=O)OC2=CC=CC(=C2)C)Cl;
	InChI InChI=1S/C14H13ClN2O4S/c1-3-22(19,20)14-16-8-11(15)12(17-14)13(18)21-10-6-4-5-9(2)7-10/h4-8H,3H2,1-2H3; Key:IJPXOPBVXVPPEW-UHFFFAOYSA-N;

SBI-115 is an experimental drug which acts as a potent and selective antagonist for the G protein-coupled bile acid receptor (GPBAR1/TGR5). It is used for studying the function of this receptor, and has been found to show beneficial effects in animal models of polycystic liver disease as well as some forms of cancer.^[1]^[2]^[3]^[4]^[5]

References

^ Masyuk TV, Masyuk AI, Lorenzo Pisarello M, Howard BN, Huang BQ, Lee PY, et al. (October 2017). "TGR5 contributes to hepatic cystogenesis in rodents with polycystic liver diseases through cyclic adenosine monophosphate/Gαs signaling". Hepatology. 66 (4). Baltimore, Md.: 1197–1218. doi:10.1002/hep.29284. PMC 5605412. PMID 28543567.
^ Lei Y, Li G, Li J, Gao S, Lei M, Gong G, et al. (June 2022). "Investigation of the potential role of TGR5 in pancreatic cancer by a comprehensive molecular experiments and the liquid chromatography mass spectrometry (LC-MS) based metabolomics". Discover Oncology. 13 (1) 46. doi:10.1007/s12672-022-00504-2. PMC 9188013. PMID 35689739.
^ Zhao Q, Ren H, Yang N, Xia X, Chen Q, Zhou D, et al. (January 2023). "Bifidobacterium pseudocatenulatum-Mediated Bile Acid Metabolism to Prevent Rheumatoid Arthritis via the Gut-Joint Axis". Nutrients. 15 (2): 255. doi:10.3390/nu15020255. PMC 9861548. PMID 36678126.
^ Li Y, Gao YN, Zhu YB, Lu WF, Yu JY, Dong YY, et al. (May 2024). "Taurocholic acid ameliorates hypertension through the activation of TGR5 in the hypothalamic paraventricular nucleus". Food & Function. 15 (9): 5088–5102. doi:10.1039/d4fo00808a. PMID 38666497.
^ Shi WG, Yao Y, Liang YJ, Lei J, Feng SY, Zhang ZX, et al. (June 2025). "Activation of TGR5 in the injured nerve site according to a prevention protocol mitigates partial sciatic nerve ligation-induced neuropathic pain by alleviating neuroinflammation". Pain. 166 (6): 1296–1313. doi:10.1097/j.pain.0000000000003460. PMC 12067609. PMID 39450924.

[1] Masyuk TV, Masyuk AI, Lorenzo Pisarello M, Howard BN, Huang BQ, Lee PY, et al. (October 2017). "TGR5 contributes to hepatic cystogenesis in rodents with polycystic liver diseases through cyclic adenosine monophosphate/Gαs signaling". Hepatology. 66 (4). Baltimore, Md.: 1197–1218. doi:10.1002/hep.29284. PMC 5605412. PMID 28543567.

[2] Lei Y, Li G, Li J, Gao S, Lei M, Gong G, et al. (June 2022). "Investigation of the potential role of TGR5 in pancreatic cancer by a comprehensive molecular experiments and the liquid chromatography mass spectrometry (LC-MS) based metabolomics". Discover Oncology. 13 (1) 46. doi:10.1007/s12672-022-00504-2. PMC 9188013. PMID 35689739.

[3] Zhao Q, Ren H, Yang N, Xia X, Chen Q, Zhou D, et al. (January 2023). "Bifidobacterium pseudocatenulatum-Mediated Bile Acid Metabolism to Prevent Rheumatoid Arthritis via the Gut-Joint Axis". Nutrients. 15 (2): 255. doi:10.3390/nu15020255. PMC 9861548. PMID 36678126.

[4] Li Y, Gao YN, Zhu YB, Lu WF, Yu JY, Dong YY, et al. (May 2024). "Taurocholic acid ameliorates hypertension through the activation of TGR5 in the hypothalamic paraventricular nucleus". Food & Function. 15 (9): 5088–5102. doi:10.1039/d4fo00808a. PMID 38666497.

[5] Shi WG, Yao Y, Liang YJ, Lei J, Feng SY, Zhang ZX, et al. (June 2025). "Activation of TGR5 in the injured nerve site according to a prevention protocol mitigates partial sciatic nerve ligation-induced neuropathic pain by alleviating neuroinflammation". Pain. 166 (6): 1296–1313. doi:10.1097/j.pain.0000000000003460. PMC 12067609. PMID 39450924.

[1]

[2]

[3]

[4]

[5]