NDB

SKU: orb1686999

Description

NDB is a potent and selective antagonist of the human farnesoid X receptor alpha (hFXRα). It effectively blocks GW4064-induced FXR/RXR heterodimerization and suppresses FXR target gene expression in primary mouse hepatocytes, making it a valuable research tool for studying metabolic diseases such as diabetes in both in vitro and in vivo models.

Research Area

Metabolism Research

Key Properties

• CAS Number: 1660153-08-1
• MW: 471.42
• Purity: 98.94% (May vary between batches)
• Formula: C₂₆H₂₈Cl₂N₂O₂
• SMILES: CN(C)c1cc(Cl)c(C(=O)N(Cc2ccccc2)c2ccc(O)c(c2)C(C)(C)C)c(Cl)c1
• Target: FXR
• Solubility: 10% DMSO+90% Corn Oil:3.3 mg/mL (7 mM);DMSO:80 mg/mL (169.7 mM)

Bioactivity

• In Vivo:
  Administered through intraperitoneal injection at a dosage of 24 mg/kg once a day for a duration of 4 weeks, NDB efficiently decreases the gene expressions of phosphoenolpyruvate carboxykinase (PEPCK), glucose 6-phosphatase (G6-pase), small heterodimer partner, and bile-salt export pump (BSEP) in db/db mice.
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• In Vitro:
  NDB induces rearrangements of helix 11 (H11) and helix 12 (H12, AF-2) by forming a homodimer of hFXRα-LBD, differing significantly from the active monomer conformation. At 25 μM, NDB effectively antagonizes the GW4064-stimulated FXR/RXR interaction and FXRα target gene expression in primary mouse hepatocytes, including the small heterodimer partner (SHP) and bile-salt export pump (BSEP).'
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

FXR

Compound Identifiers

PubChem CID

91664002