Vipoglanstat
Based on 1 Customer Validation
Vipoglanstat (BI 1029539), a carboxamide, is a potent and selective, non-peptide and orally active small molecular inhibitor of human prostaglandin E synthase 1 (mPGES-1). Vipoglanstat also has anti-inflammatory activity.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.86%
- CAS. Nr.: 1360622-01-0
- Formel: C30H34Cl2F5N5O3
- Molecular Weight:678.52
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Speicherung:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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Biologische Aktivität
Vipoglanstat significantly inhibits mPGES-1 level (IC50: about 1 nM)[3].
Vipoglanstat blocks the up-regulation of P-gp and mPGES-1 levels on glutamate-mediatedin isolated brain capillaries[3].
Vipoglanstat reduces human peripheral blood inflammatory cell migration and inflammatory mediator release[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Vipoglanstat (30 mg/kg; p.o.; 2 h, 8 h and 22 h) significantly reduces sepsis-induced BAL inflammatory cell recruitment, lung injury score and lung expression of mPGES-1 and inducible nitric oxide synthase[2].
Vipoglanstat (30 mg/kg; p.o.; QD) also significantly prolongs survival of mice with severe sepsis[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:LPS-induced acute lung injury models[2]
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Dosage:30 mg/kg
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Administration:30 mg/kg, i.p.
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Result:Preserved lung architecture and reduced immune cell influx into the lungs of LPS‑challenged mice.
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Animal Model:CLP-induced sepsis models[2]
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Dosage:30 mg/kg
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Administration:30 mg/kg, p.o., 2 hrs, 8 hrs and 22 hrs; 30 mg/kg, p.o., QD
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Result:Attenuated CLP‑induced lung injury and prolongs survival.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 1360622-01-0
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Appearance Solid
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Molecular Weight 678.52
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Formel C30H34Cl2F5N5O3
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Color White to off-white
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SMILES
CN1C2=CC(OCC(F)F)=C(C(N[C@@H]3CC[C@H](CC3)C(F)(F)F)=O)C=C2N=C1NC4=C(C(CNC(C(C)(C)C)=O)=CC=C4Cl)Cl
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Synonyms
BI 1029539; GS-248; OX-MPI
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Lösungsmittel & Löslichkeit
DMSO : 100 mg/mL (147.38 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 (sealed storage, away from moisture and light). 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 (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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.
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. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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.
Reinheit & Dokumentation
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Data Sheet (273 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
Verweise
[2]. Malarvizhi Gurusamy, et al. Inhibition of microsomal prostaglandin E synthase-1 ameliorates acute lung injury in mice. [Content Brief]
[3]. Yan-Yu Zhang, et al. Microsomal prostaglandin E 2 synthase-1 and its inhibitors: Molecular mechanisms and therapeutic significance. Pharmacol Res. 2022 Jan;175:105977. [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 (sealed storage, away from moisture and light). 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 |
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| DMSO | 1 mM | 1.4738 mL | 7.3690 mL | 14.7380 mL | 36.8449 mL |
| 5 mM | 0.2948 mL | 1.4738 mL | 2.9476 mL | 7.3690 mL | |
| 10 mM | 0.1474 mL | 0.7369 mL | 1.4738 mL | 3.6845 mL | |
| 15 mM | 0.0983 mL | 0.4913 mL | 0.9825 mL | 2.4563 mL | |
| 20 mM | 0.0737 mL | 0.3684 mL | 0.7369 mL | 1.8422 mL | |
| 25 mM | 0.0590 mL | 0.2948 mL | 0.5895 mL | 1.4738 mL | |
| 30 mM | 0.0491 mL | 0.2456 mL | 0.4913 mL | 1.2282 mL | |
| 40 mM | 0.0368 mL | 0.1842 mL | 0.3684 mL | 0.9211 mL | |
| 50 mM | 0.0295 mL | 0.1474 mL | 0.2948 mL | 0.7369 mL | |
| 60 mM | 0.0246 mL | 0.1228 mL | 0.2456 mL | 0.6141 mL | |
| 80 mM | 0.0184 mL | 0.0921 mL | 0.1842 mL | 0.4606 mL | |
| 100 mM | 0.0147 mL | 0.0737 mL | 0.1474 mL | 0.3684 mL |
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