Nidufexor (LMB763) | FXR agonist | Probechem Biochemicals

Chemical Structure : Nidufexor

CAS No.: 1773489-72-7

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Nidufexor (LMB763, LMB-763)

货号: 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).

规格	价格	库存
5 mg	￥780	In stock
10 mg	￥1180	In stock
50 mg	￥2580	In stock
100 mg	￥4280	In stock
250 mg		Get quote

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生物&药学活性

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.

物理化学性质&存储条件

分子量	487.94
分子式	C27H22ClN3O4
外观性状	Solid
CAS No.
储存条件	固体粉末 -20 °C 12 个月; 4°C 6 个月	配置液 -80 °C 6 个月; -20°C 6 个月
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

参考文献

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

Nidufexor (LMB763, LMB-763)

生物&药学活性

物理化学性质&存储条件

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Nidufexor (LMB763, LMB-763)

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物理化学性质&存储条件

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