Zaloglanstat
Based on 1 Customer Validation
Zaloglanstat (ISC-27864; GRC-27864) is a selective, orally active microsomal mPGES-1 inhibitor. Zaloglanstat has an IC50 of 5 nM for human mPGES-1 without significant inhibitory effect on COX-1/2 (IC50 >10 μM). Zaloglanstat blocks the conversion of arachidonic acid metabolite prostaglandin PGH2 to prostaglandin PGE2, thereby inhibiting inflammation-related PGE2 overproduction and reducing inflammatory responses and pain. Zaloglanstat inhibits IL-1β-induced PGE2 release in A549 cells and human synovial fibroblasts in vitro. Zaloglanstat inhibits PGE2 release in pig and dog whole blood with IC50s ??of 161 nM and 154 nM, respectively. Zaloglanstat can be used in the study of asthma, osteoarthritis, and neurodegenerative diseases.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 98.50%
- CAS. Nr.: 1513852-12-4
- Formel: C21H20ClF3N4O2
- Molecular Weight:452.86
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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
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Biologische Aktivität
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mPGES-1 |
PGE2 |
Zaloglanstat selectively inhibits human recombinant mPGES-1 activity and IL-1β potency in A549 cells with IC50 of 5 nM, and has no significant inhibition on COX-1/2 (IC50 >10 μM)[1].
Zaloglanstat inhibits (PGE2) release induced by IL-1β in A549 cells and human synovial fibroblasts in a dose-dependent manner with IC50 <10 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 1513852-12-4
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Appearance Solid
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Molecular Weight 452.86
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Formel C21H20ClF3N4O2
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Color White to off-white
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SMILES
O=C1NC(C2=C(Cl)C=CC(CNC(C(C)(C)C)=O)=C2)=NN1C3=CC=C(C(F)(F)F)C=C3
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Synonyms
ISC-27864; GRC-27864
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Lösungsmittel & Löslichkeit
DMSO : 250 mg/mL (552.05 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.
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.
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 (272 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
[1]. Zhang YY, et al. Microsomal prostaglandin E2 synthase-1 and its inhibitors: Molecular mechanisms and therapeutic significance. Pharmacol Res. 2022 Jan;175:105977. [Content Brief]
[2]. Di Micco S, et al. Identification of 2-(thiophen-2-yl)acetic Acid-Based Lead Compound for mPGES-1 Inhibition. Front Chem. 2021 May 7;9:676631. [Content Brief]
[3]. Mann MK, et al. Structure-Activity Relationship of USP5 Inhibitors [published correction appears in J Med Chem. 2022 Jan 13;65(1):889]. J Med Chem. 2021;64(20):15017-15036. [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 | 2.2082 mL | 11.0409 mL | 22.0819 mL | 55.2047 mL |
| 5 mM | 0.4416 mL | 2.2082 mL | 4.4164 mL | 11.0409 mL | |
| 10 mM | 0.2208 mL | 1.1041 mL | 2.2082 mL | 5.5205 mL | |
| 15 mM | 0.1472 mL | 0.7361 mL | 1.4721 mL | 3.6803 mL | |
| 20 mM | 0.1104 mL | 0.5520 mL | 1.1041 mL | 2.7602 mL | |
| 25 mM | 0.0883 mL | 0.4416 mL | 0.8833 mL | 2.2082 mL | |
| 30 mM | 0.0736 mL | 0.3680 mL | 0.7361 mL | 1.8402 mL | |
| 40 mM | 0.0552 mL | 0.2760 mL | 0.5520 mL | 1.3801 mL | |
| 50 mM | 0.0442 mL | 0.2208 mL | 0.4416 mL | 1.1041 mL | |
| 60 mM | 0.0368 mL | 0.1840 mL | 0.3680 mL | 0.9201 mL | |
| 80 mM | 0.0276 mL | 0.1380 mL | 0.2760 mL | 0.6901 mL | |
| 100 mM | 0.0221 mL | 0.1104 mL | 0.2208 mL | 0.5520 mL |
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