Zaltoprofen
Based on 2 publication(s) in Google Scholar
Zaltoprofen (CN100), a non-steroidal anti-inflammatory drug (NSAID), is a preferential and orally active COX-2 inhibitor, with IC50s of 1.3 and 0.34 μM for COX-1 and COX-2, respectively. Zaltoprofen exhibits powerful anti-inflammatory effects as well as an analgesic action on inflammatory pain.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 98.89%
- No. CAS: 74711-43-6
- Fòrmula: C17H14O3S
- Peso molecular:298.36
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Zaltoprofen
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
COX-2 0.34 μM (IC50) |
COX-1 1.3 μM (IC50) |
In Vitro
Zaltoprofen (0.1-10 μM; 15 min) inhibits thromboxane B2 production in human platelets in a dose-dependent manner[1].
Zaltoprofen (0.01-1 μM; 30 min) inhibits prostaglandin E2 production by interleukin-1β-stimulated synovial cells[1].
Zaltoprofen (0.1-1 μM; 5 min) inhibits the bradykinin-induced increase of [Ca2+]i in DRG cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Zaltoprofen (3-30 mg/kg; a single p.o.) inhibits the acetic acid-induced writhing response of mice in a dose-dependent manner[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Eight-week-old male Wistar rats were injected Bradykinin every 15 min[2]
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Dosage:5, 10, 20 mg/kg
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Administration:A single p.o.
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Result:Inhibited bradykinin-induced nociceptive responses, with an ED50 of 9.7 mg/kg.
The duration of analgesic effect was 60-90 min.
Ensayo clínico
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 74711-43-6
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Appearance Solid
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Peso molecular 298.36
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Fòrmula C17H14O3S
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Color White to off-white
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SMILES
CC(C1=CC=C(SC2=C3C=CC=C2)C(CC3=O)=C1)C(O)=O
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Synonyms
CN100
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
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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ACS Environ Au
Machine Learning-Assisted Recognition of Environmental Sulfur-Containing Chemicals in Nontargeted Mass Spectrometry Analysis of Inadequate Mass Resolution. [Abstract]2025 Aug 5;5(6):573-582. PMID: 41277996 -
Anal Chem
Exposome-Scale Investigation of Cl-/Br-Containing Chemicals Using High-Resolution Mass Spectrometry, Multistage Machine Learning, and Cloud Computing. [Abstract]2025 Jun 3;97(21):11099-11109. PMID: 40401576
Solvente y solubilidad
In Vitro:
DMSO : ≥ 100 mg/mL (335.17 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)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (8.38 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 (8.38 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 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.
In Vivo Dissolution Calculator
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.
Pureza y Documentación
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Ficha de datos (276 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Kawai S, et, al. Comparison of cyclooxygenase-1 and -2 inhibitory activities of various nonsteroidal anti-inflammatory drugs using human platelets and synovial cells. Eur J Pharmacol. 1998 Apr 17;347(1):87-94. [Content Brief]
[2]. Hirate K, et, al. Zaltoprofen, a non-steroidal anti-inflammatory drug, inhibits bradykinin-induced pain responses without blocking bradykinin receptors. Neurosci Res. 2006 Apr;54(4):288-94. [Content Brief]
[3]. Kameyama T, et, al. Analgesic and antiinflammatory effects of 2-(10,11-dihydro-10-oxo-dibenzo[b,f]thiepin-2-yl)propionic acid in rat and mouse. Arzneimittelforschung. 1987 Jan;37(1):19-26. [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 |
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| DMSO | 1 mM | 3.3517 mL | 16.7583 mL | 33.5166 mL | 83.7914 mL |
| 5 mM | 0.6703 mL | 3.3517 mL | 6.7033 mL | 16.7583 mL | |
| 10 mM | 0.3352 mL | 1.6758 mL | 3.3517 mL | 8.3791 mL | |
| 15 mM | 0.2234 mL | 1.1172 mL | 2.2344 mL | 5.5861 mL | |
| 20 mM | 0.1676 mL | 0.8379 mL | 1.6758 mL | 4.1896 mL | |
| 25 mM | 0.1341 mL | 0.6703 mL | 1.3407 mL | 3.3517 mL | |
| 30 mM | 0.1117 mL | 0.5586 mL | 1.1172 mL | 2.7930 mL | |
| 40 mM | 0.0838 mL | 0.4190 mL | 0.8379 mL | 2.0948 mL | |
| 50 mM | 0.0670 mL | 0.3352 mL | 0.6703 mL | 1.6758 mL | |
| 60 mM | 0.0559 mL | 0.2793 mL | 0.5586 mL | 1.3965 mL | |
| 80 mM | 0.0419 mL | 0.2095 mL | 0.4190 mL | 1.0474 mL | |
| 100 mM | 0.0335 mL | 0.1676 mL | 0.3352 mL | 0.8379 mL |
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