| Bioactivity | TP-050 is a potent, orally active and selective NMDAR agonist with an EC50 value of 0.51 µM and 9.6 µM for GluN2A and GluN2D, respecticely. TP-050 can cross the blood-brain barrier (BBB). TP-050 induces hippocampal long-term (LPT) potentiation enhancemen and enhances neuronal signal transmission[1]. |
| Target | EC50: 0.51 µM (GluN2A) and 9.6 µM (GluN2D) |
| In Vivo | TP-050 (10 mg/kg; p.o.) induces neuroplastic enhancement in Sprague-Dawley rats[1]. Animal Model: |
| Name | TP-050 |
| Formula | C16H15ClF2N6O |
| Molar Mass | 380.78 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Sakurai F, et, al. Discovery of Pyrazolo[1,5-a]pyrazin-4-ones as Potent and Brain Penetrant GluN2A-Selective Positive Allosteric Modulators Reducing AMPA Receptor Binding Activity. Bioorg Med Chem. 2022 Feb 15;56:116576. |