mPGES1-IN-7
Based on 1 Customer Validation
mPGES-1-IN-2 (compound III) is a benzimidazole-based mPGES-1 inhibitor that also inhibits adipophysin PGD synthase (I-PGDS) (5 μM, IR=60 %). mPGES-1-IN-2 reduces PGE2 production and tends to reduce levels of other prostaglandins. mPGES-1-IN-2 effectively inhibits acute inflammation in an air sac model stimulated by Carrageenan (HY-125474) in mice.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.78%
- No. CAS: 1268709-57-4
- Fòrmula: C23H34N4O
- Peso molecular:382.54
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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
Actividad biológica
IC50: 0.9 μM (recombinant human mPGES-1), 0.09 μM (recombinant rat mPGES-1)[1]; lipocalin-type PGD synthase (I-PGDS)[1]
mPGES-1-IN-2 (compound III) (0.64-80 μM; 24 h) can reduce PGE2 production after LPS (10 ng/mL) stimulation in A549 cells, mouse macrophages, and blood [1] .br/mPGES-1-IN-2 () Inhibits PGE2 synthesis in a concentration-dependent manner, causing PGH2 to shunt to the prostacyclin pathway[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:1% Carrageenan stimulated mouse air pouch model[1]
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Dosage:10, 50, 100 mg/kg
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Administration:ip; single dose after modeling: use 3 mL of sterile-filtered air was injected sub-cutaneously into the interscapular region of mice; triggered in the pouch 24 h later by the injection of a 1 ml solution of λ-carrageenan (1%) in saline.
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Result:Had no effect on inflammatory exudate volume but dose-dependently reduced cell migration.
Resulted in a decrease in PGE2 synthesis, it does not affect changes in other prostaglandin levels, but leads to an overall downregulation of prostaglandin synthesis.
Chemical Information
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No. CAS 1268709-57-4
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Appearance Solid
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Peso molecular 382.54
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Fòrmula C23H34N4O
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Color White to off-white
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SMILES
O=C(NC1CCCC1)C2CCN(CC2)C3=NC4=CC(C)=C(C=C4N3C(C)C)C
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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 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 31.25 mg/mL (81.69 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 mg/mL (5.23 mM); Clear solution
This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 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.
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 (272 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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Instrucciones de manejo (2659 KB)
Referencias
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 | 2.6141 mL | 13.0705 mL | 26.1411 mL | 65.3526 mL |
| 5 mM | 0.5228 mL | 2.6141 mL | 5.2282 mL | 13.0705 mL | |
| 10 mM | 0.2614 mL | 1.3071 mL | 2.6141 mL | 6.5353 mL | |
| 15 mM | 0.1743 mL | 0.8714 mL | 1.7427 mL | 4.3568 mL | |
| 20 mM | 0.1307 mL | 0.6535 mL | 1.3071 mL | 3.2676 mL | |
| 25 mM | 0.1046 mL | 0.5228 mL | 1.0456 mL | 2.6141 mL | |
| 30 mM | 0.0871 mL | 0.4357 mL | 0.8714 mL | 2.1784 mL | |
| 40 mM | 0.0654 mL | 0.3268 mL | 0.6535 mL | 1.6338 mL | |
| 50 mM | 0.0523 mL | 0.2614 mL | 0.5228 mL | 1.3071 mL | |
| 60 mM | 0.0436 mL | 0.2178 mL | 0.4357 mL | 1.0892 mL | |
| 80 mM | 0.0327 mL | 0.1634 mL | 0.3268 mL | 0.8169 mL |
mPGES1-IN-7 Related Classifications
HY-118282 Related Classifications
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