DY268

• CAT Number: R032751
• CAS Number: 1609564-75-1
• Molecular Formula: C30H32N4O5S
• Molecular Weight: 560.66
• Purity: ≥95%
• Synonyms: 1-[(3-methoxyphenyl)methyl]-N-(4-methyl-3-morpholin-4-ylsulfonylphenyl)-3-(4-methylphenyl)pyrazole-4-carboxamide
• InChI: InChI=1S/C30H32N4O5S/c1-21-7-10-24(11-8-21)29-27(20-33(32-29)19-23-5-4-6-26(17-23)38-3)30(35)31-25-12-9-22(2)28(18-25)40(36,37)34-13-15-39-16-14-34/h4-12,17-18,20H,13-16,19H2,1-3H3,(H,31,35)
• InChIKey: KQSPAAPFKIEUGH-UHFFFAOYSA-N
• SMILES: CC1=CC=C(C=C1)C2=NN(C=C2C(=O)NC3=CC(=C(C=C3)C)S(=O)(=O)N4CCOCC4)CC5=CC(=CC=C5)OC

DY268 is a farnesoid X receptor (FXR) antagonist (IC50=7.5 nM). It inhibits FXR transactivation in a cell-based assay with an IC50 value of 468 nM. DY268 can be used in the study of drug-induced liver injury (DILI)[1][2].
DY268 (10 μM) treatment from 13 dpf to 15 dpf increased Bhmt expression in 15-dpf Tg(fabp10a:pt-β-catenin) livers compared with DMSO treatment[2].
DY268 exhibits a>25% drop in ATP relative to vehicle-treated control at the highest concentration tested[3].

Reference

[1]. Yu DD, Lin W, Forman BM, Chen T. Identification of trisubstituted-pyrazol carboxamide analogs as novel and potent antagonists of farnesoid X receptor. Bioorg Med Chem. 2014 Jun 1;22(11):2919-38.
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[2]. Kyounghwa Jung, et al. Farnesoid X Receptor Activation Impairs Liver Progenitor Cell-Mediated Liver Regeneration via the PTEN-PI3K-AKT-mTOR Axis in Zebrafish. Hepatology. 2021 Jul;74(1):397-410.
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[3]. Leah M Norona, et al. In vitro assessment of farnesoid X receptor antagonism to predict drug-induced liver injury risk. Arch Toxicol. 2020 Sep;94(9):3185-3200.
 [Content Brief]