Piperacetazine
Based on 1 publication(s) in Google Scholar
Piperacetazine is an orally active dopamine receptor antagonist and phenothiazine antipsychotic. Piperacetazine can directly bind to the PAX3::FOXO1 fusion protein and inhibit its transcriptional activity. Piperacetazine also exhibits antitumor activity with an IC50 of 7.627 μM against PANC-1 cells. Piperacetazine can be used for the research of diseases such as schizophrenia and pancreatic cancer and other tumors.
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- Purity: 98.03%
- CAS No.: 3819-00-9
- 화학식: C24H30N2O2S
- 분자량:410.57
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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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Publications Citing Use of MedChemExpress (MCE) Piperacetazine
MoreAll Dopamine Receptor Isoforms
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Biological Activity
Piperacetazine (10 μmol/L; 6 days) downregulates the protein expression of PAX3::FOXO1 target genes MYOD1, MYOG, and B7-H3 in RH30 cells without affecting the level of PAX3::FOXO1 itself[1].
Piperacetazine (15 μmol/L; 19 days) inhibits the anchorage-independent growth of RH30 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Piperacetazine (0.005-0.025%; feed management; 1 year) is well-tolerated in rats[2].
Piperacetazine (0.25-5.0 mg/kg; oral administration; 52 weeks) is well-tolerated in dogs[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 3819-00-9
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Appearance Solid
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분자량 410.57
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화학식 C24H30N2O2S
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Color Light yellow to yellow
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SMILES
CC(C(C=C1N2CCCN3CCC(CCO)CC3)=CC=C1SC4=C2C=CC=C4)=O
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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 (1)
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Journal Impact Factor
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Most Recent
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Cancer Res Commun
Piperacetazine directly binds to the PAX3::FOXO1 fusion protein and inhibits its transcriptional activity. [Abstract]2023 Oct 6;3(10):2030-2043. PMID: 37732905
용액&용해도
Ethanol : 50 mg/mL (121.78 mM; Need ultrasonic)
DMSO : ≥ 6 mg/mL (14.61 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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% EtOH 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.09 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 EtOH 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% EtOH 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.09 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 EtOH 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 (274 KB)
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SDS (393 KB)
- English - EN (393 KB)
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- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Nakazawa K, et al. Piperacetazine Directly Binds to the PAX3::FOXO1 Fusion Protein and Inhibits Its Transcriptional Activity. Cancer Res Commun. 2023 Oct 6;3(10):2030-2043. [Content Brief]
[2]. WEAVER LC, et al. Toxicopathologic and pharmacologic properties of piperacetazine, a potent tranquilizing agent. Toxicol Appl Pharmacol. 1963 Jan;5:49-60. [Content Brief]
[3]. Deng J, et al. Identification of an autophagy-related gene signature for predicting prognosis and immune activity in pancreatic adenocarcinoma. Sci Rep. 2022 Apr 29;12(1):7006. [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 / Ethanol | 1 mM | 2.4356 mL | 12.1782 mL | 24.3564 mL | 60.8910 mL |
| 5 mM | 0.4871 mL | 2.4356 mL | 4.8713 mL | 12.1782 mL | |
| 10 mM | 0.2436 mL | 1.2178 mL | 2.4356 mL | 6.0891 mL | |
| Ethanol | 15 mM | 0.1624 mL | 0.8119 mL | 1.6238 mL | 4.0594 mL |
| 20 mM | 0.1218 mL | 0.6089 mL | 1.2178 mL | 3.0445 mL | |
| 25 mM | 0.0974 mL | 0.4871 mL | 0.9743 mL | 2.4356 mL | |
| 30 mM | 0.0812 mL | 0.4059 mL | 0.8119 mL | 2.0297 mL | |
| 40 mM | 0.0609 mL | 0.3045 mL | 0.6089 mL | 1.5223 mL | |
| 50 mM | 0.0487 mL | 0.2436 mL | 0.4871 mL | 1.2178 mL | |
| 60 mM | 0.0406 mL | 0.2030 mL | 0.4059 mL | 1.0148 mL | |
| 80 mM | 0.0304 mL | 0.1522 mL | 0.3045 mL | 0.7611 mL | |
| 100 mM | 0.0244 mL | 0.1218 mL | 0.2436 mL | 0.6089 mL |
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