A GPBAR1 antagonist
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SBI-115

Item No. 39168

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
5-chloro-2-(ethylsulfonyl)-4-pyrimidinecarboxylic acid 3-methylphenyl ester
CAS Number
882366-16-7
Molecular Formula
C14H13ClN2O4S
Formula Weight
340.8
Purity
≥98%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
Acetonitrile: Soluble
SMILES
O=C(C1=NC(S(=O)(CC)=O)=NC=C1Cl)OC2=CC=CC(C)=C2
InChi Code
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
InChi Key
IJPXOPBVXVPPEW-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $61

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    10 mg

    $109

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    25 mg

    $258

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    50 mg

    $484

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    Cayman Chemical
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    Product Description

    SBI-115 is an antagonist of G protein-coupled bile acid receptor 1 (GPBAR1), also known as TGR5.1 It inhibits taurolithocholic acid-induced increases in cAMP levels in, and proliferation of, cholangiocytes isolated from patients with autosomal dominant polycystic kidney disease when used at concentrations of 100 and 200 µM. SBI-115 (10 µM) decreases the viability of, and protein levels of GPBAR1 in, PANC-1 pancreatic cancer cells.2 In vivo, SBI-115 (80 mg/kg) prevents B. pseudocatenulatum-induced decreases in serum levels of IFN-γ and IL-17A in a mouse model of collagen-induced arthritis.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Masyuk, T.V., Masyuk, A.I., Pisarello, M.L., et al. TGR5 contributes to hepatic cystogenesis in rodents with polycystic liver diseases through cyclic adenosine monophosphate/Gαs signaling. Hepatology 66(4), 1197-1218 (2017).

    2. Lei, Y., Li, G., Li, J., et al. 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. Discov. Oncol. 13(46), (2022).

    3. Zhao, Q., Ren, H., Yang, N., et al. Bifidobacterium pseudocatenulatum-mediated bile acid metabolism to prevent rheumatoid arthritis via the gut-Joint axis. Nutrients 15(2), 255 (2023).