Oglemilast
Based on 1 Customer Validation
Oglemilast (GRC 3886) is a potent and orally active phosphodiesterase-4 (PDE4) inhibitor with an IC50 of 0.5 nM for PDE4D3. Oglemilast inhibits pulmonary cell infiltration, including eosinophilia and neutrophilia in vitro and in vivo. Oglemilast has the potential for inflammatory airway diseases.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit : 99.97%
- CAS. Nr.: 778576-62-8
- Formel: C20H13Cl2F2N3O5S
- Molecular Weight:516.30
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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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HY-16900
RolipramPDE4 Inhibitor -
HY-15455
RoflumilastPDE4 Inhibitor -
HY-10978
CrisaborolePDE Inhibitor -
HY-12085
ApremilastPDE-4 Inhibitor -
HY-10790
CilomilastPDE4 Inhibitor -
HY-16900R
Rolipram (Standard)Reference Standard -
HY-15485
ZardaverinePDE3/4 Inhibitor -
HY-10978R
Crisaborole (Standard)PDE Inhibitor -
HY-10469
GSK256066Phosphodiesterase 4 Inhibitor -
HY-16578
GW9662PPARγ Antagonist -
HY-17386
RosiglitazonePPARγ Agonist -
HY-B0392
(S)-(+)-RolipramPDE4 Inhibitor
Biologische Aktivität
Beschreibung
IC50 & Target
[3]|
PDE4D3 .5 nM (IC50) |
In Vitro
Oglemilast (GRC 3886) has EC50s of 11.4 nM, 4.4 nM for PDE 4B1 and PDE 4D3 reporter cell lines, respectively[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 778576-62-8
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Appearance Solid
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Molecular Weight 516.30
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Formel C20H13Cl2F2N3O5S
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Color Off-white to light yellow
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SMILES
O=C(C1=C2C(OC3=CC=C(NS(=O)(C)=O)C=C23)=C(OC(F)F)C=C1)NC4=C(Cl)C=NC=C4Cl
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Synonyms
GRC 3886
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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 2 years -20°C 1 year
Lösungsmittel & Löslichkeit
In Vitro:
DMSO : 4 mg/mL (7.75 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, 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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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.
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.
Reinheit & Dokumentation
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Data Sheet (282 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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Handling Instructions (2659 KB)
Verweise
[1]. Giembycz MA. Can the anti-inflammatory potential of PDE4 inhibitors be realized: guarded optimism or wishful thinking? Br J Pharmacol. 2008 Oct;155(3):288-90. [Content Brief]
[2]. Rabe KF, et al. Update on roflumilast, a phosphodiesterase 4 inhibitor for the treatment of chronic obstructive pulmonary disease. Br J Pharmacol. 2011 May;163(1):53-67. [Content Brief]
[3]. Wunder F, et al. Characterization of the cellular activity of PDE 4 inhibitors using two novel PDE 4 reporter celllines. Mol Pharm. 2013 Oct 7;10(10):3697-705. [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 | 1.9369 mL | 9.6843 mL | 19.3686 mL | 48.4215 mL |
| 5 mM | 0.3874 mL | 1.9369 mL | 3.8737 mL | 9.6843 mL |
Oglemilast Related Classifications
HY-15178 Related Classifications
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