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TUG-770

In stock
Catalog No.
A3895
FFA1/GPR40 agonist
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$255.00
In stock
5mg
$233.00
In stock
10mg
$355.00
In stock
25mg
$514.00
In stock
50mg
$841.00
In stock

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Email: [email protected]

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Background

IC50: 6 nM

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].

Clinical trial: N/A

Reference:
[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.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt307.32
Cas No.1402601-82-4
FormulaC19H14FNO2
SynonymsTUG770;TUG 770
Solubility≥11.85 mg/mL in DMSO, ≥9.5 mg/mL in EtOH with ultrasonic and warming, <2.41 mg/mL in H2O
Chemical Name3-[4-[2-[2-(cyanomethyl)phenyl]ethynyl]-2-fluorophenyl]propanoic acid
SDFDownload SDF
Canonical SMILESC1=CC=C(C(=C1)CC#N)C#CC2=CC(=C(C=C2)CCC(=O)O)F
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Quality Control

Chemical structure

TUG-770