TUG-770 Chemical Properties

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

TUG-770 Usage And Synthesis

Uses

TUG-770 is a potent, selective and orally active GPR40/FFA1 agonist with an EC50 of 6 nM for human FFA1. TUG-770 shows a high selectivity for FFA1 over FFA2, FFA3, FFA4, PPARγ, other receptors, transporters, and enzymes. TUG-770 can be uesd for type 2 diabetes research[1]. TUG-770 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

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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