TGN-020

- Overview
  - TGN-020 (TGN020) is a novel and potent inhibitor of aquaporin 4 (AQP4) channel (IC50: 3.1 μM), which is the most abundant water channel in the brain. It acts by increasing regional cerebral blood flow and reducing ischemia-induced brain edema. Aquaporin 4 (AQP4), the most abundant isozyme of the water specific membrane transporter aquaporin family, has now been implicated to play a significant role in the pathogenesis of various disease processes of the nervous system from epilepsy to Alzheimer's disease. Considering its clinical relevance, it is highly desirable to develop a noninvasive method for the quantitative analysis of AQP distribution in humans under clinical settings. Currently, the method of choice for such diagnostic examinations continues to be positron emission tomography (PET). Here, we report the successful development of a PET ligand for AQP4 imaging based on TGN-020, a potent AQP4 inhibitor developed previously in our laboratory. Utilizing [(11)C]-TGN-020, PET images were successfully generated in wild type and AQP4 null mice, providing a basis for future evaluation regarding its suitability for clinical studies.
    
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- Properties
  - Categories
    
    PROTAC Linkers
    
    CAS Number
    
    51987-99-6
    
    Molecular Formula
    
    C8H6N4OS
    
    Molecular Weight
    
    206.22
    
    Purity
    
    ≥98%
    
    Storage
    
    Powder: store in -20°C freezer for up to three years, store in 4°C freezer for up to two years
    In solvent: store in -80°C freezer for up to six months, store in -20°C freezer for up to two months
    
    Shipping
    
    Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
    
    SMILES
    
    O=C(C1=CC=CN=C1)NC2=NN=CS2
    
    * For research use only

TGN-020

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