1. GPCR/G Protein
  2. GPR52
  3. TP-024

TP-024 est un agoniste de GPR52 qui est sélectif avec un EC50 de 75 nM. TP-024 possède des propriétés antipsychotiques et procognitives.

TP-024 (FTBMT) is a selective GPR52 agonist with an EC50 of 75 nM. TP-024 has antipsychotic and procognitive properties.

For research use only. We do not sell to patients.

TP-024 Chemical Structure

TP-024 Chemical Structure

CAS No. : 1358575-02-6

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Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products

1 Publications Citing Use of MCE TP-024

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

TP-024 (FTBMT) is a selective GPR52 agonist with an EC50 of 75 nM[1]. TP-024 has antipsychotic and procognitive properties[2].

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 pEC50s of 7.03, 6.85, and 6.87, respectively[2].

MedChemExpress (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].

MedChemExpress (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].
Molecular Weight

392.35

Formula

C19H16F4N4O

CAS No.
Appearance

Solid

Color

Light yellow to orange

SMILES

O=C(N)C1=CC=C(N2C(C)=NC(CC3=CC(C(F)(F)F)=CC(F)=C3)=N2)C=C1C

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
In Vitro: 

DMSO : 50 mg/mL (127.44 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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C2

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Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (5.30 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.08 mg/mL (5.30 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

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(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.96%

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.5487 mL 12.7437 mL 25.4874 mL 63.7186 mL
5 mM 0.5097 mL 2.5487 mL 5.0975 mL 12.7437 mL
10 mM 0.2549 mL 1.2744 mL 2.5487 mL 6.3719 mL
15 mM 0.1699 mL 0.8496 mL 1.6992 mL 4.2479 mL
20 mM 0.1274 mL 0.6372 mL 1.2744 mL 3.1859 mL
25 mM 0.1019 mL 0.5097 mL 1.0195 mL 2.5487 mL
30 mM 0.0850 mL 0.4248 mL 0.8496 mL 2.1240 mL
40 mM 0.0637 mL 0.3186 mL 0.6372 mL 1.5930 mL
50 mM 0.0510 mL 0.2549 mL 0.5097 mL 1.2744 mL
60 mM 0.0425 mL 0.2124 mL 0.4248 mL 1.0620 mL
80 mM 0.0319 mL 0.1593 mL 0.3186 mL 0.7965 mL
100 mM 0.0255 mL 0.1274 mL 0.2549 mL 0.6372 mL
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TP-024 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
TP-024
Cat. No.:
HY-101787
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