SBI-115

Last updated

SBI-115
SBI-115 structure.png
Identifiers
  • (3-methylphenyl) 5-chloro-2-ethylsulfonylpyrimidine-4-carboxylate
CAS Number
PubChem CID
ChemSpider
Chemical and physical data
Formula C14H13ClN2O4S
Molar mass 340.78 g·mol−1
3D model (JSmol)
  • CCS(=O)(=O)C1=NC=C(C(=N1)C(=O)OC2=CC=CC(=C2)C)Cl
  • 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

  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.