An FXR agonist
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HPG1860

Item No. 39481

Technical Information
Formal Name
2-[(2R)-4-[[5-cyclopropyl-3-(2,6-dichlorophenyl)-4-isoxazolyl]methyl]-2-methyl-1-piperazinyl]-4-methoxy-6-benzothiazolecarboxylic acid
CAS Number
2226133-29-3
Molecular Formula
C27H26Cl2N4O4S
Formula Weight
Purity
≥98%
Formulation
A neat solid
DMSO: Sparingly soluble: 1-10 mg/mlEthanol: Sparingly soluble: 1-10 mg/ml
SMILES
COC1=C2C(SC(N3CCN(CC4=C(C5CC5)ON=C4C6=C(Cl)C=CC=C6Cl)C[C@H]3C)=N2)=CC(C(O)=O)=C1
InChi Code
InChI=1S/C27H26Cl2N4O4S/c1-14-12-32(8-9-33(14)27-30-24-20(36-2)10-16(26(34)35)11-21(24)38-27)13-17-23(31-37-25(17)15-6-7-15)22-18(28)4-3-5-19(22)29/h3-5,10-11,14-15H,6-9,12-13H2,1-2H3,(H,34,35)/t14-/m1/s1
InChi Key
JPEHHEUXHNQIIX-CQSZACIVSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    HPG1860 is a farnesoid X receptor (FXR) agonist.1 It induces luminescence in a reporter assay using HEK293T cells expressing human FXR (EC50 = 18 nM). In vivo, HPG1860 (1, 3, or 10 mg/kg per day) decreases the serum levels of alanine transaminase (ALT) and total cholesterol, as well as hepatic inflammation, fat levels, and fibrosis, in a mouse model of non-alcoholic steatohepatitis (NASH) induced by a high-fat diet and carbon tetrachloride (CCl4).

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Mo, C., Xu, X., Zhang, P., et alDiscovery of HPG1860, a structurally novel nonbile acid FXR agonist currently in clinical development for the treatment of nonalcoholic steatohepatitis. J. Med. Chem. 66(14), 9363-9375 (2023).