| Description | TM-N1324 is a GPR39 agonist. 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 to murine GPR39 with EC50s of 180 nM and 5 nM, respectively. |
| In vitro | 测量结果证实，GPR39激动剂TM-N1324能使生长抑素的释放增加53%。TM-N1324显示出具有前景的体外ADME特性。此外，TM-N1324在pH 7.0时具有相当好的水溶性（65 μM）[1]。 |
| Target activity | GPR39 without Zn2+ (human):280 nM (EC50), GPR39 without Zn2+ (murine):180 nM (EC50), GPR39 with Zn2+ (human):9 nM (EC50), GPR39 with Zn2+ (murine):5 nM (EC50) |
| molecular weight | 397.79 |
| Molecular formula | C18H13ClFN7O |
| CAS | 1144477-35-9 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility | DMSO: 10 mg/mL (25.14 mM), Sonication and heating are recommended. |
| References | 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. |