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| Targets |
TP-10 targets phosphodiesterase 10A (PDE10A), an enzyme that hydrolyzes both cAMP and cGMP. By inhibiting PDE10A, it increases the levels of cAMP and cGMP in cells, particularly in the striatum, which enhances the responsiveness of striatal neurons to electrical stimulation. This makes it a target for neurological research.
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| ln Vitro |
Total reactive oxygen species in human brain-derived cells (U-87 MG) are impacted by TP-10 (10 μg/mL; 24 hours) [3].
In vitro, TP-10 demonstrates potent PDE10A inhibitory activity with an IC50 of 0.8 nM. It also shows antioxidant activity. Its high selectivity for PDE10A over other PDEs makes it a valuable tool for studying the specific role of PDE10A in cellular signaling. |
| ln Vivo |
On cyclic nucleotides, TP-10 (0.1–10 mg/kg; once an hour) has demonstrated effects [2].
In vivo, TP-10 is active in the mouse behavioral model for positive symptoms. It increases the responsiveness of striatal neurons to electrical stimulation of the ipsilateral frontal cortex. It has been studied for its potential in treating neurological diseases, such as schizophrenia and Huntington's disease. |
| Enzyme Assay |
The in vitro enzyme assay for TP-10 involves measuring its ability to inhibit PDE10A activity. The enzyme is incubated with a substrate (e.g., cAMP or cGMP) in the presence of varying concentrations of the compound. The amount of product (e.g., AMP or GMP) is measured using a luminescent or fluorescent detection system, and the IC50 is calculated from the dose-response curve.
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| Cell Assay |
Cell viability assay [3]
Cell Types: U-87 MG Cell Tested Concentrations: 10 μg/ml Incubation Duration: 24 hrs (hours) Experimental Results: The total number of ROS-positive cells diminished, and there was no toxic effect on U-87 MG cells. In vitro cell culture studies for TP-10 utilize neuronal cell lines or primary neurons. Cells are treated with the compound, and the levels of cAMP and cGMP are measured by ELISA or a radioimmunoassay. The phosphorylation of downstream targets, such as CREB, is analyzed by Western blotting to confirm PDE10A inhibition. |
| Animal Protocol |
Animal/Disease Models: Male CD rat [2]
Doses: 0.1, 0.32, 1.0, 3.2 and 10 mg/kg Route of Administration: subcutaneous injection; 0.1-10 mg/kg One-time Experimental Results: Dose- and time-dependent increase in striae in mice cGMP and cAMP levels in the body. Three hrs (hrs (hours)) after injection at a dose of 3.2 mg/kg, pCREB-LI levels first increased and returned to basal levels. In vivo animal experiments for TP-10 have been performed in mouse models of positive symptoms. In these studies, the compound is administered, and behavioral parameters are assessed. Its effects on striatal neuron responsiveness are studied by electrophysiology. Its efficacy in models of neurological diseases, such as the R6/2 mouse model of Huntington's disease, can also be assessed. |
| ADME/Pharmacokinetics |
TP-10 has a molecular formula of C26H19F3N4O and a molecular weight of 460.45 g/mol. It is a solid compound that is soluble in DMSO. It is typically stored as a powder at -20°C for long-term stability. Its stability is maintained under recommended storage conditions. It has a predicted density of 1.42±0.1 g/cm3.
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| Toxicity/Toxicokinetics |
Toxicological data for TP-10 are limited, as it is a research compound. In vitro, it has been shown to have antioxidant activity, suggesting it may have a protective effect. However, it is not intended for human use. Comprehensive toxicity studies have not been reported. Standard safety precautions for handling chemical reagents should be followed.
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| References |
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| Additional Infomation |
TP-10 is a research compound with no clinical approval. It is a valuable tool for studying PDE10A biology and the role of PDE10A in neurological and psychiatric disorders. It is used in drug discovery programs to explore the therapeutic potential of PDE10A inhibitors for the treatment of schizophrenia, Huntington's disease, and other neurological conditions.
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| Molecular Formula |
C26H19N4OF3
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| Molecular Weight |
460.45046
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| Exact Mass |
460.151
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| CAS # |
898563-00-3
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| PubChem CID |
11648276
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| Appearance |
Light yellow to brown solid powder
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| LogP |
6.301
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
34
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| Complexity |
636
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=CC=C2C(=C1)C=CC(=N2)COC3=CC=C(C=C3)C4=NN(C=C4C5=CC=NC=C5)CC(F)(F)F
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| InChi Key |
NOIXNOMHHWGUTG-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C26H19F3N4O/c27-26(28,29)17-33-15-23(18-11-13-30-14-12-18)25(32-33)20-6-9-22(10-7-20)34-16-21-8-5-19-3-1-2-4-24(19)31-21/h1-15H,16-17H2
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| Chemical Name |
2-[[4-[4-pyridin-4-yl-1-(2,2,2-trifluoroethyl)pyrazol-3-yl]phenoxy]methyl]quinoline
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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 |
| 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 : ~100 mg/mL (~217.18 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (5.43 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.43 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 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. View More
Solubility in Formulation 3: ≥ 2.38 mg/mL (5.17 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. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1718 mL | 10.8589 mL | 21.7179 mL | |
| 5 mM | 0.4344 mL | 2.1718 mL | 4.3436 mL | |
| 10 mM | 0.2172 mL | 1.0859 mL | 2.1718 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.
Link: https://clinicaltrials.gov/ct2/show/NCT02302755
Conditions:Dense Deposit DiseaseLink: https://clinicaltrials.gov/ct2/show/NCT00082121
Conditions:Myocardial Ischemia|Coronary Arteriosclerosis|Aortic Valve Insufficiency|Mitral Valve InsufficiencyProducts are for research use only; We do not sell to patients
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