Name: TUG-770
Price: 436.00 USD

- Overview
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    Background
    
    IC50: 6 nMTUG-770 is a potent free fatty acid receptor 1 (FFA1/GPR40) agonist. Free fatty acid receptor 1 (FFA1 or GPR40) enhances the glucose-stimulated insulin secretion from pancreatic β-cells and attracts high interest as a new target for the treatment of type 2 diabetes. In vitro: TUG-770 showed a pronounced increase in potency on FFA1 with EC50 = 6 nM and 150-fold selectivity over FFA4. TUG-770 showed a high selectivity over FFA2, FFA3, PPARγ, and 54 diverse transporters, receptors, and enzymes. In the rat INS-1E cell line, TUG-770 caused significantly increased insulin secretion at high glucose concentration and, as expected, no effect at low glucose concentration [1]. In vivo: Pharmacokinetic studies of TUG-770 in mice showed a fast oral absorption, higher plasma concentration, a longer half-life, lower clearance, and increased bioavailability. No adverse effects were seen in mice after four weeks of daily oral treatment of 20 mg/kg and acute treatment in doses up to 250 mg/kg. In vivo examination of TUG-770 in an acute intraperitoneal glucose tolerance test in normal mice showed a good dose-dependent response with maximal reduction in glucose level reached at 50 mg/kg. The followed chronic oral glucose tolerance test study in DIO mice showed that TUG-770 was more effective than its analog. Further evaluation of TUG-770 in rats confirmed a significant glucose lowering effect for the high doses [1]. Clinical trial: N/A
- Properties
  - Categories
    
    FFA1/GPR40 agonist
    
    Alternative Name
    
    TUG770;TUG 770; 3-[4-[2-[2-(cyanomethyl)phenyl]ethynyl]-2-fluorophenyl]propanoic acid
    
    CAS Number
    
    1402601-82-4
    
    Molecular Formula
    
    C19H14FNO2
    
    Molecular Weight
    
    307.32
    
    Appearance
    
    A solid
    
    Purity
    
    99.46%
    
    Solubility
    
    insoluble in H2O; ≥11.85 mg/mL in DMSO; ≥9.5 mg/mL in EtOH with gentle warming and ultrasonic
    
    Storage
    
    Store at -20°C
    
    SMILES
    
    C1=CC=C(C(=C1)CC#N)C#CC2=CC(=C(C=C2)CCC(=O)O)F
    
    * For Research Use Only