| Description | TC-N 22A is a strong, selective, oral active mGlu4 forward allosteric regulator (PAM) that can cross the blood-brain barrier. EC50 expression of TC-N 22A in BHK cells expressing human mGlu4 was 9 nM. TC-N 22A showed very low activity against mGlu 1, 2, 3, 5, and 7 receptors in excitation and forward allosteric models (EC50 >10 μM). TC-N 22A can be used in the study of central nervous system diseases. |
| Target activity | mGlu1/2/3/5/7 receptors:>10 μM (EC50), mGlu4 receptor:9 nM (EC50) |
| molecular weight | 283.35 |
| Molecular formula | C14H13N5S |
| CAS | 1314140-00-5 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 50 mg/mL (176.46 mM) |
| References | 1. Sang-Phyo Hong, et al. Tricyclic thiazolopyrazole derivatives as metabotropic glutamate receptor 4 positive allosteric modulators. J Med Chem. 2011 Jul 28;54(14):5070-81. |