[CAS NO. 1358575-02-6] TP-024
PRODUCTS SPECIFICATIONS [1358575-02-6]
DESCRIPTION [1358575-02-6]
Overview
| MDL | MFCD31693831 |
|---|---|
| Molecular Weight | 392.35 |
| Molecular Formula | C19H16F4N4O |
| SMILES | O=C(N)C1=CC=C(N2C(C)=NC(CC3=CC(C(F)(F)F)=CC(F)=C3)=N2)C=C1C |
Summary
IC50 & Target
IC50: 75 nM (GPR52) [1]
In Vitro
TP-024 (FTBMT) (0.1-10 μM) increases intracellular cAMP levels in CHO cells expressing human, mouse, or rat GPR52, with pEC 50 s of 7.03, 6.85, and 6.87, respectively [2] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Viability Assay [1]
| 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] . |
In Vivo
TP-024 (FTBMT) (30 mg/kg, 90 minutes) exhibits antipsychotic-like activity without causing catalepsy in mice [2] .
TP-024 (3 or 10 mg/kg, 48 hours) improves recognition and spatial working memory in rats [2] .
TP-024 (3, 10, 30 mg/kg, 2 hours) stimulates neuronal activity in brain regions related to cognition [2] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Male Long-Evans rats (9 weeks old) [2] |
| Dosage: | 10 mg/kg |
| Administration: | Oral, 1 hour before memory test |
| Result: | A 1-hour pretreatment with FTBMT (10 mg/kg, p.o.) significantly decreases the number of memory errors induced by MK-801 [2] . |
| Animal Model: | Male ICR mice (7 to 8 weeks old) [2] |
| Dosage: | 3–30 mg/kg |
| Administration: | Oral, 60 minutes before s.c. administration of MK-801 |
| Result: | FTBMT increases phospho-DARPP32 levels in the NAc slices [2] . |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvent & Solubility
DMSO : 50 mg/mL ( 127.44 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 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 |
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Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.08 mg/mL (5.30 mM); Clear solution
References
- [1] Tokumaru K, et al. 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] Nishiyama K, et al. 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.