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GPR39-C3 is the first potent, selective and orally bioavailable GPR39 agonist with an EC₅₀ ~0.8 nM for human GPR39 and ~0.4 nM for rodent GPR39. It has no inhibitory effects (at 10 μM) on a panel of kinases and exhibits no relevant binding affinity for the related ghrelin and neurotensin-1 receptors and other enzymes, transporters, and GPCRs. GPR39-C3 has excellent functional activity in physiologically relevant rodent cells and in vivo. An acute study in normal mice with orally administrated GPR39-C3 confirmed in vitro findings by demonstrating an increase of the relevant pharmacodynamic marker GLP-1. It is a good chemical tool to enable interrogation of GPR39 signaling in different cellular contexts.

How to Use:

• In vitro:  GPR39-C3 was used at 0.1-1 µM final concentration in various in vitro assays.
• In vivo: GPR39-C3 was dosed to Male C57BL/6 mice via oral gavage at 30 mg/kg, concurrently with DPP4 inhibitor PKF275-055 (3 mg/kg). The animals were challenged orally after 1 hour with a glucose bolus (3 g/kg) and active GLP-1 levels were measured 30 min later by MSD Active GLP-1 Assay kit. Formulation is 0.5% methylcellulose/0.1% Tween 80 in water. 

Reference:

• 1. Stefan Peukert, et al. Discovery of 2-Pyridylpyrimidines as the First Orally Bioavailable GPR39 Agonists.  (2014) ACS Med. Chem. Lett. In press.
• 2. Bassilana F, et al. Target identification for a Hedgehog pathway inhibitor reveals the receptor GPR39. (2014) Nat Chem Biol. 10(5):343-9.