Pelubiprofen
Based on 1 Customer Validation
Pelubiprofen is an orally active anti-inflammatory agent that inhibits COX enzyme activity (with IC50 values of 10.66 and 2.88 μM for COX-1 and COX-2, respectively). Pelubiprofen has significant anti-inflammatory and analgesic effects.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté: 98.46%
- CAS No.: 69956-77-0
- Formule: C16H18O3
- Masse moléculaire:258.31
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
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Help & FAQs
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Activité biologique
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COX-2 |
TAK1 |
Pelubiprofen (0.01-60 μM, 24 h) inhibits COX in RAW 264.7 cells and suppresses LPS (HY-D1056)-induced PGE2 (IC50 is 0.13 μM)[1].
Pelubiprofen (15-60 μM, 24 h) inhibits the expression of iNOS and pro-inflammatory cytokines induced by LPS (HY-D1056) in RAW 264.7 cells[1].
Pelubiprofen (15-60 μM, 24 h) suppresses the activation of NF-κB induced by LPS (HY-D1056) in RAW 264.7 cells[1].
Pelubiprofen (15-60 μM, 24 h) inhibits IKK and TAK1 in RAW 264.7 cells induced by LPS (HY-D1056)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:RAW 264.7
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Concentration:0.01, 0.1, 1, 5, 15, 30, 60 μM
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Incubation Time:24h; 5 and 10 min
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Result:Inhibited the expression of COX-2 and PGE2, without affecting COX-1. Suppressed the expression of iNOS and reduced the levels of TNF-α, IL-1b, and IL-6.
Decreased the phosphorylation and degradation of IκB-α, inhibiting IKK and TAK1.
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Cell Line:RAW 264.7
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Concentration:15, 30, 60 μM
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Incubation Time:24h
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Result:Inhibited the expression of iNOS and reduced the levels of TNF-α, IL-1b, and IL-6.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Carrageenan-induced paw edema model [1]
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Dosage:25 and 100 mg/kg, single dose
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Administration:Oral gavage (p.o.)
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Result:Significantly reduced MPO activity, decreased production of PGE2, and notably inhibited the nuclear translocation of p65.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 69956-77-0
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Appearance Solid
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Masse moléculaire 258.31
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Formule C16H18O3
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Color White to off-white
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SMILES
O=C(O)C(C)C1=CC=C(/C=C2C(CCCC/2)=O)C=C1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
DMSO : 100 mg/mL (387.13 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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 (9.68 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 (9.68 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.
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.
Pureté et documentation
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Fiche technique (274 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Ji-Sun Shin, et al. Anti-inflammatory effect of pelubiprofen, 2-[4-(oxocyclohexylidenemethyl)-phenyl]propionic acid, mediated by dual suppression of COX activity and LPS-induced inflammatory gene expression via NF-κB inactivation. J Cell Biochem. 2011 Dec;112(12):3594-603. [Content Brief]
[2]. Choi IA, Baek HJ, et al. Comparison of the efficacy and safety profiles of a pelubiprofen versus celecoxib in patients with rheumatoid arthritis: a 6-week, multicenter, randomized, double-blind, phase III, non-inferiority clinical trial. BMC Musculoskelet Disord. 2014 Nov 18;15:375. [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, 6 months; -20°C, 1 month. 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 | 3.8713 mL | 19.3566 mL | 38.7132 mL | 96.7829 mL |
| 5 mM | 0.7743 mL | 3.8713 mL | 7.7426 mL | 19.3566 mL | |
| 10 mM | 0.3871 mL | 1.9357 mL | 3.8713 mL | 9.6783 mL | |
| 15 mM | 0.2581 mL | 1.2904 mL | 2.5809 mL | 6.4522 mL | |
| 20 mM | 0.1936 mL | 0.9678 mL | 1.9357 mL | 4.8391 mL | |
| 25 mM | 0.1549 mL | 0.7743 mL | 1.5485 mL | 3.8713 mL | |
| 30 mM | 0.1290 mL | 0.6452 mL | 1.2904 mL | 3.2261 mL | |
| 40 mM | 0.0968 mL | 0.4839 mL | 0.9678 mL | 2.4196 mL | |
| 50 mM | 0.0774 mL | 0.3871 mL | 0.7743 mL | 1.9357 mL | |
| 60 mM | 0.0645 mL | 0.3226 mL | 0.6452 mL | 1.6130 mL | |
| 80 mM | 0.0484 mL | 0.2420 mL | 0.4839 mL | 1.2098 mL | |
| 100 mM | 0.0387 mL | 0.1936 mL | 0.3871 mL | 0.9678 mL |
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