Name: KT182
Price: 266.00 USD

- Overview
  - Please contact us at for specific academic pricing.
    
    Background
    
    IC50: < 5 nMKT182 is an ABHD6 inhibitor.α/β-Hydrolase domain containing 6 (ABHD6), a transmembrane serine hydrolase, hydrolyzes the endogenous cannabinoid 2-arachidonoylglycerol (2-AG) to regulate certain forms of cannabinoid receptor-dependent signaling in the nervous system. In vitro: The in-vitro potencies were tested for KT182 and the results found that KT182 could potently inhibit ABHD6 as measured by gelbased competitive ABPP and 2-AG hydrolysis assays. Moreover, the in-situ potencies were measured by treating Neuro2A cells with varying concentrations of KT182 for 4 h, and it was found that KT182 could inhibit ABHD6 with IC50 values in the subnanomolar range [1]. In vivo: In animal study, mice were treated intraperitoneally with KT182 at various doses (0.1-1 mg/kg) for 4 h, and the results found that KT182 could produce near-complete blockade of ABHD6 in the liver at the highest dose tested. Moreover, KT182 at lower doses maintained around 80% inhibition of ABHD6 in the liver and KT182 at higher doses showed impressive selectivity in the mouse liver, exhibiting little cross-reactivity against the numerous carboxylesterase enzymes. In addition, KT182 could also completely inactivate ABHD6 in the mouse brain at 1 mg/kg [1]. Clinical trial: Up to now, KT182 is still in the preclinical development stage.
- Properties
  - Alternative Name
    
    [4-[3'-(hydroxymethyl)[1,1'-biphenyl]-4-yl]-1H-1,2,3-triazol-1-yl](2-phenyl-1-piperidinyl)-methanone
    
    CAS Number
    
    1402612-62-7
    
    Molecular Formula
    
    C27H26N4O2
    
    Molecular Weight
    
    438.5
    
    Appearance
    
    A crystalline solid
    
    Purity
    
    98.00%
    
    Solubility
    
    ≤10mg/ml in DMSO;10mg/ml in dimethyl formamide
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only

KT182

KT182

Background

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