An FXR partial agonist
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LMB763

Item No. 30184

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-[[[(8-chloro-1,4-dihydro-1-methyl[1]benzopyrano[4,3-c]pyrazol-3-yl)carbonyl](phenylmethyl)amino]methyl]-benzoic acid
CAS Number
1773489-72-7
Synonyms
  • Nidufexor
Molecular Formula
C27H22ClN3O4
Formula Weight
487.9
Purity
≥98%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMSO: solubleEthanol: soluble
λmax
232 nm
SMILES
ClC1=CC=C(OCC2=C3N(C)N=C2C(N(CC4=CC=CC=C4)CC5=CC=C(C(O)=O)C=C5)=O)C3=C1
InChi Code
InChI=1S/C27H22ClN3O4/c1-30-25-21-13-20(28)11-12-23(21)35-16-22(25)24(29-30)26(32)31(14-17-5-3-2-4-6-17)15-18-7-9-19(10-8-18)27(33)34/h2-13H,14-16H2,1H3,(H,33,34)
InChi Key
JYTIXGYXBIBOMN-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    10 mg

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    25 mg

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    Cayman Chemical
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    OBESITY RESEARCH SOLUTIONS
    Product Description

    LMB763 is a partial agonist of the farnesoid X receptor (FXR; EC50 = 7 nM).1 It is selective for FXR over a panel of enzymes, ion channels, nuclear receptors, and G protein-coupled receptors, including the androgen receptor, estrogen receptor α (ERα), and G protein-coupled bile acid receptor 1 (GPBAR1; EC50s = >30, >30, and >80 µM, respectively). LMB763 induces expression of the FXR target genes encoding the bile salt export pump and short heterodimer partner in isolated rat hepatocytes in a concentration-dependent manner. It decreases non-alcoholic fatty liver disease (NAFLD) scores and liver fibrosis in a rat model of non-alcoholic steatohepatitis (NASH).

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Chianelli, D., Rucker, P.V., Roland, J., et al. Nidufexor (LMB763), a novel FXR modulator for the treatment of nonalcoholic steatohepatitis (NASH). J. Med. Chem. 63(8), 3868-3880 (2020).