TM-N1324

TM-N1324 is an agonist of G-Protein-Coupled Receptor 39 (GPR39) with EC₅₀s of 9 nM/5 nM in the presence of Zn²⁺, and 280 nM/180 nM in the absence of Zn²⁺ for human/murine GPR39. IC50 & Target: EC50: 280 nM (human GPR39 without Zn²⁺), 9 nM (human GPR39 with Zn²⁺), 180 nM (murine GPR39 without Zn²⁺), 5 nM (murine GPR39 with Zn²⁺)^[1] In Vitro: TM-N1324 activates human GPR39 with high efficacy and potencies of 280 nM and 9 nM in the absence and presence of Zn²⁺, respectively. TM-N1324 has similar potencies on murine GPR39, 180 nM and 5 nM. TM-N1324 is also found to have promising in vitro ADME properties. TM-N1324 has reasonably good aqueous solubility (65 μM at pH 7.0). Measurements of somatostatin confirms that the GPR39 agonist TM-N1324 increases somatostatin release by 53%^[1].