| Identification | Back Directory | [Name]
TUG-770 | [CAS]
1402601-82-4 | [Synonyms]
TUG-770
CS-1047
TUG770; TUG 770
4-[2-[2-(Cyanomethyl)phenyl]ethynyl]-2-fluorobenzenepropanoic acid
3-(4-((2-(Cyanomethyl)phenyl)ethynyl)-2-fluorophenyl)propanoic acid
Benzenepropanoic acid, 4-[2-[2-(cyanomethyl)phenyl]ethynyl]-2-fluoro-
4-[2-[2-(Cyanomethyl)phenyl]ethynyl]-2-fluorobenzenepropanoic acid TUG-770 | [Molecular Formula]
C19H14FNO2 | [MDL Number]
MFCD26142679 | [MOL File]
1402601-82-4.mol | [Molecular Weight]
307.32 |
| Chemical Properties | Back Directory | [Boiling point ]
523.5±50.0 °C(Predicted) | [density ]
1.28±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
insoluble in H2O; ≥11.85 mg/mL in DMSO; ≥9.5 mg/mL in EtOH with gentle warming and ultrasonic | [form ]
solid | [pka]
4.61±0.10(Predicted) | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Biological Activity]
tug-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]. | [IC 50]
6 nm | [References]
[1] christiansen e,hansen sv,urban c,hudson bd,wargent et,grundmann m,jenkins l,zaibi m,stocker cj,ullrich s,kostenis e,kassack mu,milligan g,cawthorne ma,ulven t. discovery of tug-770: a highly potent free fatty acid receptor 1 (ffa1/gpr40) agonist for treatment of type 2 diabetes. acs med chem lett.2013 may 9;4(5):441-445. |
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