| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
GPR52 ( IC50 = 75 nM )
FTBMT targets GPR52, an orphan G protein-coupled receptor. GPR52 is expressed in the brain and is thought to play a role in psychiatric disorders. By acting as an agonist of GPR52 (EC50 = 75 nM), FTBMT activates downstream signaling pathways that produce antipsychotic and procognitive effects. It is selective for GPR52 over a panel of 98 targets. |
|---|---|
| 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].
In vitro, FTBMT is a selective GPR52 agonist with an EC50 of 75 nM. It activates GPR52 with an Emax of 122%. It shows selectivity for GPR52 over D1, D2, AMPA, and NMDA receptors. Its activity has been characterized in receptor functional assays. |
| 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]. In vivo, FTBMT has antipsychotic and procognitive effects in rodents. It inhibits MK-801-induced hyperactivity. It shows antipsychotic and recognitive properties without causing catalepsy. These effects suggest its potential as a therapeutic agent for schizophrenia. |
| Enzyme Assay |
In vitro receptor binding and functional assays for FTBMT measure its agonistic activity at GPR52. The compound is incubated with cells expressing GPR52, and receptor activation is measured by changes in cAMP levels or other downstream signaling events. The EC50 is determined from dose-response curves.
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| 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].
In vitro cell-based assays for FTBMT are not typically performed. Its activity is characterized by its receptor binding and functional profile. Its effects on neuronal signaling can be studied in cell culture models. |
| Animal Protocol |
Male Long-Evans rats (9 weeks old)
10 mg/kg Oral, 1 hour before memory test In vivo animal experiments for FTBMT have been conducted in rodent models of schizophrenia. Animals are treated with FTBMT, and its effects on MK-801-induced hyperactivity are measured. Its antipsychotic and procognitive effects are assessed using behavioral tests. |
| ADME/Pharmacokinetics |
FTBMT has a molecular weight of 392.35 and a molecular formula of C19H16F4N4O. Its exact mass is 392.126. Its purity is ≥98%. It is typically stored at -20°C.
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| Toxicity/Toxicokinetics |
FTBMT is for research use only and is not intended for human use. Its safety profile is being evaluated in preclinical studies. As a GPR52 agonist, its toxicity is related to its mechanism of action. Standard safety precautions should be taken when handling.
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| References |
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| Additional Infomation |
Selective GPR52 agonist; structure described in the first article.
FTBMT (TP-024) is a potent, selective, and orally bioavailable GPR52 agonist. It has an EC50 of 75 nM. It has antipsychotic and procognitive properties. It inhibits MK-801-induced hyperactivity without causing catalepsy. It is being investigated as a potential therapeutic agent for schizophrenia. |
| Molecular Formula |
C19H16F4N4O
|
|---|---|
| Molecular Weight |
392.350157737732
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| Exact Mass |
392.13
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| Elemental Analysis |
C, 58.16; H, 4.11; F, 19.37; N, 14.28; O, 4.08
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| CAS # |
1358575-02-6
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| PubChem CID |
56649300
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| Appearance |
Light yellow to orange solid powder
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| LogP |
4.2
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
7
|
| Rotatable Bond Count |
4
|
| Heavy Atom Count |
28
|
| Complexity |
561
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC1=C(C=CC(=C1)N2C(=NC(=N2)CC3=CC(=CC(=C3)F)C(F)(F)F)C)C(=O)N
|
| InChi Key |
TYXSIXOYTBHZFA-UHFFFAOYSA-N
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| 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
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| Synonyms |
FTBMT
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
DMSO: ~50 mg/mL (~127.4 mM)
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|---|---|
| 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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