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FXR antagonist 1

FXR antagonist 1 (compound F6) is an orally active and selective intestinal FXR antagonist (IC50=2.1 μM) . FXR antagonist 1 selectively inhibits intestinal FXR signalling through antagonism of intestinal FXR and feedback activation of hepatic FXR to improve hepatic steatosis, inflammation and fibrosis in NASH (nonalcoholic steatohepatitis) models. FXR antagonist 1 can be used in NASH studies[1].

Product Specifications

CAS Number

2295804-68-9

UNSPSC

12352211

Target

FXR

Type

Reference compound

Related Pathways

Metabolic Enzyme/Protease

Applications

Metabolism-sugar/lipid metabolism

Field of Research

Metabolic Disease

Assay Protocol

https://www.medchemexpress.com/fxr-antagonist-1.html

Purity

98.01

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

OC(CNC([C@]12[C@@]([C@@H](CC2)C(C)C)([H])[C@]3([H])[C@@](CC1)([C@]4([C@]([C@@]5([C@@](C(C)([C@@H](CC5)OC(CCC)=O)C)([H])CC4)C)([H])CC3)C)C)=O)=O

Molecular Formula

C36H59NO5

Molecular Weight

585.86

References & Citations

[1]Zhang C, et al. Discovery of Betulinic Acid Derivatives as Potent Intestinal Farnesoid X Receptor Antagonists to Ameliorate Nonalcoholic Steatohepatitis. J Med Chem. 2022 Sep 15.

Shipping Conditions

Room Temperature

Storage Conditions

-20°C, 3 years; 4°C, 2 years (Powder)

Scientific Category

Reference compound1

Clinical Information

No Development Reported

Available Sizes

Frequently Asked Questions

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