GSK256066
Based on 2 publication(s) in Google Scholar
GSK256066 is a selective and high-affinity phosphodiesterase 4 (PDE4) inhibitor, with an IC50 of 3.2 pM for PDE4B. GSK256066 is developed for the research of chronic obstructive pulmonary disease.
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- Pureza: 98.69%
- No. CAS: 801312-28-7
- Fòrmula: C27H26N4O5S
- Peso molecular:518.58
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Chemical Information
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Solvente y solubilidad
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Publications Citing Use of MedChemExpress (MCE) GSK256066
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Actividad biológica
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PDE4 3.2 pM (IC50) |
GSK256066 is an exceptionally high-affinity inhibitor of PDE4 designed for inhaled administration[1].
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GSK256066 is highly selective for PDE4, with >380,000-fold versus PDE1/2/3/5/6 and >2500-fold against PDE7[1].
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GSK256066 inhibits PDE4 isoforms A-D with equal affinity (PDE4B: pIC50≥ 11.5, PDE4A: pIC50≥11.31, PDE4C: pIC50≥11.42, PDE4D: pIC50≥11.94)[1].
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GSK256066 inhibits TNF-α production by lipopolysaccharide (LPS)-stimulated human peripheral blood monocytes with IC50 of 0.01 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
? GSK256066 also inhibits LPS-induced increases in exhaled nitric oxide (ED50=92 μg/kg)[2].
? GSK256066 inhibits pulmonary eosinophilia in rats exposed to ovalbumin (ED50=0.4 μg/kg)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Brown Norway rats (180-200 g)[2]
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Dosage:10 μg/kg
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Administration:Intratracheal injection; before (36 hours, 24 hours, 18 hours, 12 hours, 6 hours, and 2 hours) and after (0 hour, 2 hours) LPS challenge
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Result:Inhibited the LPS-induced pulmonary neutrophilia.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 801312-28-7
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Appearance Solid
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Peso molecular 518.58
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Fòrmula C27H26N4O5S
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Color Light yellow to yellow
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SMILES
O=C(N)C1=C(C2=CC(S(=O)(C3=CC=CC(C(N(C)C)=O)=C3)=O)=CC(C)=C2N=C1)NC4=CC=CC(OC)=C4
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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 2 years -20°C 1 year
Publications (2)
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Journal Impact Factor
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Most Recent
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Br J Pharmacol
Dual pharmacological targeting of coactivator-associated arginine methyltransferase 1 (CARM1) and salt inducible kinase (SIK) drives ketogenesis in both hepatocytes and mice. [Abstract]2026 Apr 29. PMID: 42055601 -
Int Immunopharmacol
MiR-124-3p targeting PDE4B attenuates LPS-induced ALI through the TLR4/NF-κB signaling pathway. [Abstract]2022 Apr:105:108540. PMID: 35063752
Solvente y solubilidad
DMSO : 25 mg/mL (48.21 mM; ultrasonic and warming and heat to 60°C; 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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureza y Documentación
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Ficha de datos (276 KB)
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SDS (644 KB)
- English - EN (644 KB)
- Français - FR (644 KB)
- Deutsch - DE (644 KB)
- Norwegian - NO (644 KB)
- Español - ES (644 KB)
- Swedish - SV (644 KB)
- Italian - IT (644 KB)
- Korean - KR (644 KB)
- Portuguese - PT (644 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Tralau-Stewart CJ, et al. GSK256066, an exceptionally high-affinity and selective inhibitor of phosphodiesterase 4 suitable for administration by inhalation: in vitro, kinetic, and in vivo characterization. J Pharmacol Exp Ther, 2011, 337(1), 145-154. [Content Brief]
[2]. Nials AT, et al. In vivo characterization of GSK256066, a high-affinity inhaled phosphodiesterase 4 inhibitor. J Pharmacol Exp Ther, 2011, 337(1), 137-144. [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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.9283 mL | 9.6417 mL | 19.2834 mL | 48.2086 mL |
| 5 mM | 0.3857 mL | 1.9283 mL | 3.8567 mL | 9.6417 mL | |
| 10 mM | 0.1928 mL | 0.9642 mL | 1.9283 mL | 4.8209 mL | |
| 15 mM | 0.1286 mL | 0.6428 mL | 1.2856 mL | 3.2139 mL | |
| 20 mM | 0.0964 mL | 0.4821 mL | 0.9642 mL | 2.4104 mL | |
| 25 mM | 0.0771 mL | 0.3857 mL | 0.7713 mL | 1.9283 mL | |
| 30 mM | 0.0643 mL | 0.3214 mL | 0.6428 mL | 1.6070 mL | |
| 40 mM | 0.0482 mL | 0.2410 mL | 0.4821 mL | 1.2052 mL |
GSK256066 Related Classifications
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