TUG-770 Struktur

TUG-770

Bezeichnung:TUG-770

CAS-Nr1402601-82-4

Englisch Name:TUG-770

CBNumberCB42659732

SummenformelC19H14FNO2

Molgewicht307.32

MOL-Datei1402601-82-4.mol

TUG-770 physikalisch-chemischer Eigenschaften

Siedepunkt	523.5±50.0 °C(Predicted)
Dichte	1.28±0.1 g/cm3(Predicted)
storage temp.	Store at -20°C
Löslichkeit	insoluble in H2O; ≥11.85 mg/mL in DMSO; ≥9.5 mg/mL in EtOH with gentle warming and ultrasonic
Aggregatzustand	solid
pka	4.61±0.10(Predicted)
Farbe	Light yellow to yellow

TUG-770 Chemische Eigenschaften,Einsatz,Produktion Methoden

Biologische Aktivität
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
Einzelnachweise
[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.

TUG-770 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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