Nidufexor |CAS:1773489-72-7 Probechem Biochemicals

Chemical Structure : Nidufexor

CAS No.: 1773489-72-7

Nidufexor (LMB763, LMB-763)

Catalog No.: PC-61390Not For Human Use, Lab Use Only.

Nidufexor (LMB763, LMB-763) is a potent, selective, non-bile acid partial agonist of farnesoid X receptor (FXR) with EC50 of 7 nM in FXR-HTRF biochemical assay measuring the ligand-induced interaction between FXR and the Steroid Receptor Coactivator-1 (SRC1).

Packing	Price	Stock
5 mg	$128	In stock
10 mg	$188	In stock
25 mg	$298	In stock
50 mg	$488	In stock
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Biological Activity

Nidufexor (LMB763, LMB-763) is a potent, selective, non-bile acid partial agonist of farnesoid X receptor (FXR) with EC50 of 7 nM in FXR-HTRF biochemical assay measuring the ligand-induced interaction between FXR and the Steroid Receptor Coactivator-1 (SRC1).

Nidufexor (LMB763) displays no activation of other nuclear receptors such as AR, ERα, GR, PPARγ, PR, or PXR using a TR-FRET assay (EC50 > 30 μM) and no activation of RXR, LXR, GR, PPARγ, or ERα using a cell-based agonist assay (EC50 > 10 μM).

Nidufexor (LMB763) exhibits EC50 of 32 nM in cell-based FXR BSEP-luciferase reporter assays.

Nidufexor (LMB763) induces BSEP mRNA levels ∼3.7-fold compared to DMSO control, in rat primary hepatocytes, which is 100-fold lower potency than tropifexor.

Nidufexor (LMB763) (1.5 mg/kg, oral gavage, once daily for 14 days) exhibits statistically significant 3.5-fold increase in serum FGF15 protein levels in Han-Wistar rats.

Nidufexor (LMB763) (3, 10, 30 mg/kg) reduces NASH activity scores and limits liver fibrosis in NASH murine model.

Physicochemical Properties

M.Wt	487.94
Formula	C27H22ClN3O4
Appearance	Solid
CAS No.
Storage	Solide Powder -20 °C 12 Months; 4°C 6 Months	In Solvent -80 °C 6 Months; -20°C 6 Months
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	4-[(N-benzyl-8-chloro-1-methyl-1,4-dihydro[1]benzopyrano[4,3-c]pyrazole-3-carboxamido)methyl]benzoic acid

References

1. Chianelli D, et al. J Med Chem. 2020 Apr 23;63(8):3868-3880.

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Nidufexor (LMB763, LMB-763)

Biological Activity

Physicochemical Properties

References

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