1144477-35-9

EC50: 280 nM (human GPR39 without Zn ²⁺ ), 9 nM (human GPR39 with Zn ²⁺ ), 180 nM (murine GPR39 without Zn ²⁺ ), 5 nM (murine GPR39 with Zn ²⁺ )

TM-N1324 activates human GPR39 with high efficacy and potencies of 280 nM and 9 nM in the absence and presence of Zn ²⁺ , 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%.