TM-N1324是G蛋白偶联受体39(GPR39)的激动剂，在Zn2+存在的情况下，对人和鼠GPR39的EC50值分别为9nM和5nM，在Zn2+不存在的情况下，对人和鼠GPR39的EC50值分别为280nM和180nM。
CAS：1144477-35-9
分子式：C18H13ClFN7O
分子量：397.79
纯度：98%
存储：Store at -20°C

Background:

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.

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].

[1]. Frimurer TM, et al. Model-Based Discovery of Synthetic Agonists for the Zn2+-Sensing G-Protein-Coupled Receptor 39 (GPR39) Reveals Novel Biological Functions. J Med Chem. 2017 Feb 9;60(3):886-898.