MI-883

Overview

MI-883 is orally active constitutive androstane receptor (CAR) ( EC 50 of 73 nM) agonist and pregnane X Receptor (PXR) ( IC 50 of 100 nM) antagonist. MI-883 binds to CAR and PXR ligand-binding domains, promotes CAR LBD assembly, activates CAR3 variant, stimulates CAR cytoplasmic-nuclear translocation, upregulates CAR target genes, recruits coactivators NCOA1, NCOA2, NCOA3, inhibits basal and agonist-induced PXR activation, downregulates PXR target genes, disrupts PXR-NCOR2 interaction, blocks agonist-mediated PXR-NCOA1 recruitment. MI-883 reduces plasma total cholesterol , LDL cholesterol , and hepatic free cholesterol levels, increases fecal bile acid excretion, regulates genes involved in xenobiotic metabolism, cholesterol homeostasis, and bile acid homeostasis. MI-883 exhibits metabolic stability, liver-predominant distribution, a safety profile with no observed toxicity, and does not stimulate human hepatocyte hypertrophy or hyperplasia. MI-883 can be used for the research of diet-induced hypercholesterolemia.

Application

Products | Products > Disease Areas > Metabolic or Endocrine Disease | Products > Disease Areas > Lipid Metabolism | Products > Disease Areas > Hypercholesterolemia | Products > Signaling Pathways > Vitamin D Related/Nuclear Receptor | Products > Signaling Pathways > Metabolic Enzyme/Protease | Products > Research Areas > Metabolic Disease | Products > Signaling Pathways > Constitutive Androstane Receptor | Products > Signaling Pathways > Pregnane X Receptor (PXR) | Products > Signaling Pathways > Cytochrome P450

Product Information

• Catalog No.: HY-173033
• CAS No.: 2530027-71-3
• Molecular Formula: C23H15Cl2FN6O
• Molecular Weight: 481.31
• Purity: 99.57%
• Storage: Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
• Availability: In-stock

Source

Original product source