TUG-424 

TUG-424 is a potent and selective free fatty acid receptor 1 (FFA1/GPR40) agonist with an EC₅₀ of 32 nM. TUG-424 significantly increases glucose-stimulated insulin secretion at 100 nM. TUG-424 may serve to explore the role of FFA1 in metabolic diseases such as diabetes or obesity^[1]. TUG-424 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

EC50: 32 nM (FFA1/GPR40)^[1]

Increasing concentrations (100 nM to 10 µM) of TUG-424 enhances glucose-stimulated insulin secretion significantly already at 100 nM and with a maximal effect at 3 µM. The approximately 2-fold stimulation of secretion by TUG-424 in the presence of 12 mM glucose is comparable to that induced by palmitate in the presence of the same glucose concentration. Basal insulin secretion at 2.8 mM glucose is slightly but significantly reduces by TUG-424^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

264.32

C₁₈H₁₆O₂

1082058-99-8

Solid

White to off-white

OC(CCC(C=C1)=CC=C1C#CC2=C(C)C=CC=C2)=O

Room temperature in continental US; may vary elsewhere.

• [1]. Discovery of Potent and Selective Agonists for the Free Fatty Acid Receptor 1 (FFA1/GPR40), a Potential Target for the Treatment of Type II Diabetes J. Med. Chem., 2008, 51 (22), pp 7061-7064

  [2]. Christiansen E, et al. Discovery of potent and selective agonists for the free fatty acid receptor 1 (FFA(1)/GPR40), a potential target for the treatment of type II diabetes. J Med Chem. 2008 Nov 27;51(22):7061-4.  [Content Brief]