An FXR agonist and inhibitor of FABP1
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ZLY28

Item No. 38864

Technical Information
Formal Name
1-[4′-[[5-cyclopropyl-3-(2,6-dichlorophenyl)-4-isoxazolyl]methoxy][1,1′-biphenyl]-3-yl]-cyclopropanecarboxylic acid
CAS Number
3004676-77-8
Molecular Formula
C29H23Cl2NO4
Formula Weight
Purity
≥90%
Formulation
A solid
DMF: 30 mg/mlDMSO: 30 mg/mlEthanol: 30 mg/ml
λmax
265 nm
SMILES
ClC1=CC=CC(Cl)=C1C2=NOC(C3CC3)=C2COC4=CC=C(C5=CC=CC(C6(CC6)C(O)=O)=C5)C=C4
InChi Code
InChI=1S/C29H23Cl2NO4/c30-23-5-2-6-24(31)25(23)26-22(27(36-32-26)18-7-8-18)16-35-21-11-9-17(10-12-21)19-3-1-4-20(15-19)29(13-14-29)28(33)34/h1-6,9-12,15,18H,7-8,13-14,16H2,(H,33,34)
InChi Key
GFQRXOXNBQDNBC-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    Product Description

    ZLY28 is a farnesoid X receptor (FXR) agonist and an inhibitor of fatty acid binding protein 1 (FABP1).1 It selectively induces reporter gene expression in HepG2 cells expressing human FXR (EC50 = 143 nM) over cells expressing 19 other receptors (EC50s = >10,000 nM for all). ZLY28 selectively inhibits FABP1 (IC50 = 2.7 µM) over FABP3 (IC50 = >30 µM) but also inhibits FABP4 (IC50 = 6.3 µM). In vivo, ZLY28 (20 mg/kg) induces FXR-related gene expression in the ileum but not the liver in a mouse model of carbon tetrachloride-induced non-alcoholic steatohepatitis (NASH). It also reduces hepatocyte ballooning, as well as hepatic lobular inflammation and steatosis in the same model.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Ren, Q., Chen, Y., Zhou, Z., et alDiscovery of the first-in-class intestinal restricted FXR and FABP1 dual modulator ZLY28 for the treatment of nonalcoholic fatty liver disease. J. Med. Chem. 66(9), 6082-6104 (2023).