Name: BIM5078
Price: 209.00 USD

- Overview
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    Background
    
    EC50: 11.9 nM for HNF4αBIM5078 is a HNF4α antagonist.Hepatocyte nuclear factor (HNF)4α is a key regulator of gene expression in cell types playing a important role in metabolic homeostasis, such as hepatocytes, enterocytes, as well as pancreatic β cells.In vitro: The EC50 of BIM5078 was calculated to be 11.9 nM and further analyses of the data using the Hill equation showed that the Hill coefficient for BIM5078 was 0.9, consistent with a single binding complex between BIM5078 and HNF4α. In docking study, the high GoldScore indicated that it was reasonable for BIM5078 to bind in the LBP in a position similar to that of the putative endogenous ligand. Moreover, BIM5078 could potently repress HNF4α expression in T6PNE, the murine insulinoma cell line MIN6, and in the HepG2 hepatoma line, which had exceptionally high levels of HNF4α expression [1]. In vivo: BI6015, a analog of BIM5078, could induce a loss of HNF4α protein in the liver, but not in the intestine or kidney, which was consistent with the in vitro effects of BIM5078 on HNF4α expression both in human- and murine-derived cell lines. In addition, no difference in the cell number expressing the proliferation marker Ki67 was observed in liver, intestine, or kidney with BI6015, when compared with vehicle-treated animals [1]. Clinical trial: Up to now, BIM5078 is still in the preclinical development stage.
- Properties
  - Categories
    
    HNF4α antagonist
    
    Alternative Name
    
    1-[(2-chloro-5-nitrophenyl)sulfonyl]-2-methyl-1H-benzimidazole
    
    CAS Number
    
    337506-43-1
    
    Molecular Formula
    
    C14H10ClN3O4S
    
    Molecular Weight
    
    351.8
    
    Appearance
    
    A crystalline solid
    
    Purity
    
    98.00%
    
    Solubility
    
    ≤5mg/ml in DMSO;3mg/ml in dimethyl formamide
    
    Storage
    
    Store at -20°C
    
    SMILES
    
    CC1=NC2=CC=CC=C2N1S(C3=C(Cl)C=CC([N+]([O-])=O)=C3)(=O)=O
    
    * For Research Use Only

Documents

COA (Certificate Of Analysis)

MSDS (Material Safety Data Sheet)

Datasheet

BIM5078

BIM5078

Background

Documents

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