FTBMT is a novel, potent, selective and orally bioavailable GPR52 agonist with antipsychotic and procognitive properties. With an EC50 value of 75 nM, it activates GPR52.
Physicochemical Properties
| Molecular Formula | C19H16F4N4O |
| Molecular Weight | 392.350157737732 |
| Exact Mass | 392.13 |
| Elemental Analysis | C, 58.16; H, 4.11; F, 19.37; N, 14.28; O, 4.08 |
| CAS # | 1358575-02-6 |
| PubChem CID | 56649300 |
| Appearance | Light yellow to orange solid powder |
| LogP | 4.2 |
| Hydrogen Bond Donor Count | 1 |
| Hydrogen Bond Acceptor Count | 7 |
| Rotatable Bond Count | 4 |
| Heavy Atom Count | 28 |
| Complexity | 561 |
| Defined Atom Stereocenter Count | 0 |
| InChi Key | TYXSIXOYTBHZFA-UHFFFAOYSA-N |
| InChi Code | InChI=1S/C19H16F4N4O/c1-10-5-15(3-4-16(10)18(24)28)27-11(2)25-17(26-27)8-12-6-13(19(21,22)23)9-14(20)7-12/h3-7,9H,8H2,1-2H3,(H2,24,28) |
| Chemical Name | 4-[3-[[3-fluoro-5-(trifluoromethyl)phenyl]methyl]-5-methyl-1,2,4-triazol-1-yl]-2-methylbenzamide |
| Synonyms | FTBMT |
| HS Tariff Code | 2934.99.9001 |
| Storage |
Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| Shipping Condition | Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs) |
Biological Activity
| Targets | GPR52 ( IC50 = 75 nM ) |
| ln Vitro | TP-024 (FTBMT) (0.1-10 μM) raises intracellular cAMP levels in CHO cells expressing human, mouse, or rat GPR52, with pEC50s of 7.03, 6.85, and 6.87, respectively[2]. |
| ln Vivo |
TP-024 (FTBMT) (30 mg/kg, 90 minutes) shows antipsychotic-like effects without inducing catalepsy in mice[2]. TP-024 (3 or 10 mg/kg, 48 hours) enhances spatial working memory and recognition in rats[2]. TP-024 (3, 10, 30 mg/kg, 2 hours) stimulates neuronal activity in brain regions linked to cognition[2]. |
| Cell Assay | Cell Line: CHO cells (expressing GPR52 receptors) cAMP assay Concentration: 0.1-10 μM Incubation Time: 30 minutes Result: FTBMT activated cAMP signaling in vitro[1]. |
| Animal Protocol |
Male Long-Evans rats (9 weeks old) 10 mg/kg Oral, 1 hour before memory test |
| References |
[1]. Design, synthesis, and pharmacological evaluation of 4-azolyl-benzamide derivatives as novel GPR52 agonists. Bioorg Med Chem. 2017 Jun 15;25(12):3098-3115. [2]. FTBMT, a Novel and Selective GPR52 Agonist, Demonstrates Antipsychotic-Like and Procognitive Effects in Rodents, Revealing a Potential Therapeutic Agent for Schizophrenia. J Pharmacol Exp Ther. 2017 Nov;363(2):253-264. |
Solubility Data
| Solubility (In Vitro) | DMSO: ~50 mg/mL (~127.4 mM) |
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.30 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (5.30 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5487 mL | 12.7437 mL | 25.4874 mL | |
| 5 mM | 0.5097 mL | 2.5487 mL | 5.0975 mL | |
| 10 mM | 0.2549 mL | 1.2744 mL | 2.5487 mL |