TUG-770 is a highly potent agonist of free fatty acid receptor 1 (FFA1/GPR40, EC50: 6 nM for hFFA1).

TUG-770 (Compound 22) displayed excellent physicochemical and in vitro ADME properties, with good aqueous solubility, good chemical stability, low lipophilicity, and decreased plasma protein binding (PPB). TUG-770 furthermore showed excellent stability toward human liver microsomes, no inhibition of selected CYP-enzymes implicated in drug-drug interactions, no P-glycoprotein inhibition, and good permeability in the Caco-2 cell assay.

Examination of TUG-770 in an acute intraperitoneal glucose tolerance test (IPGTT) in normal mice revealed a good dose-dependent response with maximal reduction in glucose level reached at 50 mg/kg. The effect of TUG-770 was fully sustained after 29 days of daily oral treatment. Additional evaluation of TUG-770 in rats confirmed a significant glucose-lowering effect for the high doses already after 10 min and for all doses after 30 min.

1402601-82-4

C19H14FNO2

307.32

H2O:Insoluble
DMSO:100 mg/mL (325.39 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years