Name: Adaptaquin
Price: 247.00 USD

- Overview
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    Background
    
    Adaptaquin is a selective hydroxyquinoline HIF prolyl hydroxylase (HIF-PHD) inhibitor [1][2].
    The hypoxia-inducible factor prolyl hydroxylase domain enzymes (HIF-PHDs) are a family of oxygen sensors that has been implicated in neuronal survival. Catalysis by the HIF-PHDs destabilizes the transcriptional activator HIF-1a under normoxia. HIF-PHDs are promising target candidates for mitochondrial protection in paradigms of oxidative stress. The inhibition of HIF-PHDs prevented neuronal cell death induced by mitochondrial toxins [1][2].
    Adaptaquin is a hydroxyquinoline HIF-PHD inhibitor. Adaptaquin inhibited purified and recombinant PHD2. Adaptaquin (30 mg/kg) penetrated the blood-brain barrier, resulting in inhibition of the oxygen-sensing HIF-PHDs and activation of HIF-dependent gene expression [1]. In HT-22 cells, Adaptaquin protected against glutamate-induced cell death. Adaptaquin could also restore the mitochondrial ATP production [2].
    In intracerebral hemorrhage (ICH) mice model, Adaptaquin decreased edema and significantly improved tape removal task, which were associated with a reduction in the number of degenerating neurons in perihematomal and hematomal areas of the mouse striatum [1].
    
    [1]. Karuppagounder SS, Alim I, Khim SJ, et al. Therapeutic targeting of oxygen-sensing prolyl hydroxylases abrogates ATF4-dependent neuronal death and improves outcomes after brain hemorrhage in several rodent models. Sci Transl Med. 2016 Mar 2;8(328):328ra29.
    [2]. Neitemeier S, Dolga AM, Honrath B, et al. Inhibition of HIF-prolyl-4-hydroxylases prevents mitochondrial impairment and cell death in a model of neuronal oxytosis. Cell Death Dis. 2016 May 5;7:e2214.
- Properties
  - Alternative Name
    
    HIF prolyl hydroxylase inhibitor; 7-[(4-chlorophenyl)[(3-hydroxy-2-pyridinyl)amino]methyl]-8-quinolinol
    
    CAS Number
    
    385786-48-1
    
    Molecular Formula
    
    C21H16ClN3O2
    
    Molecular Weight
    
    377.8
    
    Appearance
    
    A crystalline solid
    
    Purity
    
    Purity ≥ 95.00%
    
    Solubility
    
    ≤30mg/ml in DMSO;30mg/ml in dimethyl formamide
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only