TP-10
Based on 2 publication(s) in Google Scholar
TP-10 is a selective PDE10A inhibitor with an IC50 value of 0.8 nM. TP-10 shows an antioxidant activity with IC50s of 31.72 and 16.04 μg/ml for DPPH and CUPRAC, respectively. TP-10 can be used for the research of neuropathy.
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- Purity: 99.95%
- CAS No.: 898563-00-3
- 화학식: C26H19F3N4O
- 분자량:460.45
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) TP-10
More
Biological Activity
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PDE10 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Sf9 | IC50 |
1.41 nM
Compound: 13
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Inhibition of rat recombinant PDE10A transfected in Sf9 cells
Inhibition of rat recombinant PDE10A transfected in Sf9 cells
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[PMID: 19630403] |
TP-10 (10 μg /mL; 24 h) affects total reactive oxygen species in human brain-derived cells (U-87 MG)[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:U-87 MG cells
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Concentration:10 μg/ml
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Incubation Time:24 hours
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Result:Decreased the total number of ROS-positive cells and showed no toxic effects to U-87 MG cells.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male CD rats[2]
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Dosage:0.1, 0.32, 1.0, 3.2 and 10 mg/kg
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Administration:Subcutaneous injection; 0.1-10 mg/kg once
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Result:Dose- and time-dependently increased the levels of both cGMP and cAMP in striatal of mice. Increased pCREB-LI level first and returned to basal levels after injected for 3 hours at a dose of 3.2 mg/kg.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 898563-00-3
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Appearance Solid
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분자량 460.45
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화학식 C26H19F3N4O
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Color Light yellow to brown
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SMILES
FC(F)(F)CN1C=C(C2=CC=NC=C2)C(C(C=C3)=CC=C3OCC4=NC5=CC=CC=C5C=C4)=N1
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (2)
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Journal Impact Factor
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Most Recent
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Nat Commun
Inhalable cardiac targeting peptide modified nanomedicine prevents pressure overload heart failure in male mice. [Abstract]2024 Jul 18;15(1):6058. PMID: 39025877 -
용액&용해도
DMSO : 100 mg/mL (217.18 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.43 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (5.43 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
순도&문서
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Data Sheet (275 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Portuguese - PT (254 KB)
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Handling Instructions (2659 KB)
References
[1]. Hamaguchi W, et al. Synthesis and in vivo evaluation of novel quinoline derivatives as phosphodiesterase 10A inhibitors. Chem Pharm Bull (Tokyo). 2014;62(12):1200-1213. [Content Brief]
[2]. Schmidt CJ, et al. Preclinical characterization of selective phosphodiesterase 10A inhibitors: a new therapeutic approach to the treatment of schizophrenia. J Pharmacol Exp Ther. 2008 May;325(2):681-90. [Content Brief]
[3]. Kaproń B, et al. 1,2,4-Triazole-based anticonvulsant agents with additional ROS scavenging activity are effective in a model of pharmacoresistant epilepsy. J Enzyme Inhib Med Chem. 2020 Dec;35(1):993-1002. [Content Brief]
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.1718 mL | 10.8589 mL | 21.7179 mL | 54.2947 mL |
| 5 mM | 0.4344 mL | 2.1718 mL | 4.3436 mL | 10.8589 mL | |
| 10 mM | 0.2172 mL | 1.0859 mL | 2.1718 mL | 5.4295 mL | |
| 15 mM | 0.1448 mL | 0.7239 mL | 1.4479 mL | 3.6196 mL | |
| 20 mM | 0.1086 mL | 0.5429 mL | 1.0859 mL | 2.7147 mL | |
| 25 mM | 0.0869 mL | 0.4344 mL | 0.8687 mL | 2.1718 mL | |
| 30 mM | 0.0724 mL | 0.3620 mL | 0.7239 mL | 1.8098 mL | |
| 40 mM | 0.0543 mL | 0.2715 mL | 0.5429 mL | 1.3574 mL | |
| 50 mM | 0.0434 mL | 0.2172 mL | 0.4344 mL | 1.0859 mL | |
| 60 mM | 0.0362 mL | 0.1810 mL | 0.3620 mL | 0.9049 mL | |
| 80 mM | 0.0271 mL | 0.1357 mL | 0.2715 mL | 0.6787 mL | |
| 100 mM | 0.0217 mL | 0.1086 mL | 0.2172 mL | 0.5429 mL |
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