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GSK356278
🥰Excellent
Catalog No. T27475Cas No. 720704-34-7
Alias GSK-356278, GSK 356278
GSK356278 is an effective and selective inhibitor of phosphodiesterase 4 (PDE4), with pIC50s of 8.6, 8.8, and 8.7 for human PDE4A, PDE4B, and PDE4D, respectively. GSK356278 has anti-inflammatory, anxiolytic, and cognition-enhancing effects.
GSK356278
🥰Excellent
Purity: 99.43%
Catalog No. T27475Alias GSK-356278, GSK 356278Cas No. 720704-34-7
GSK356278 is an effective and selective inhibitor of phosphodiesterase 4 (PDE4), with pIC50s of 8.6, 8.8, and 8.7 for human PDE4A, PDE4B, and PDE4D, respectively. GSK356278 has anti-inflammatory, anxiolytic, and cognition-enhancing effects.
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 2 mg | 32 € | In Stock | |
| 5 mg | 52 € | In Stock | |
| 10 mg | 84 € | In Stock | |
| 25 mg | 164 € | In Stock | |
| 50 mg | 305 € | In Stock | |
| 100 mg | 487 € | In Stock | |
| 200 mg | 663 € | In Stock | |
| 500 mg | 1.035 € | In Stock |
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Purity:99.43%
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All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.Product Introduction
Bioactivity
Chemical Properties
| Description | GSK356278 is an effective and selective inhibitor of phosphodiesterase 4 (PDE4), with pIC50s of 8.6, 8.8, and 8.7 for human PDE4A, PDE4B, and PDE4D, respectively. GSK356278 has anti-inflammatory, anxiolytic, and cognition-enhancing effects. |
| Targets&IC50 | PDE4B:8.8 (pIC50), PDE4D:8.7 (pIC50), PDE4A:8.6 (pIC50) |
| In vitro | GSK356278 bounds to the HARBS in rats, mice, marmosets, and ferrets with pKis of 7.9, 7.8, 8.4, and 8.5, respectively. GSK356278 inhibits LPS-induced release of TNF-α in human whole blood, with a pIC50 of 7.6. GSK356278 competes with [3H]rolipram for the high affinity rolipram binding site (HARBS) with a pKi of 8.6 in a competitive filtration-binding assay to the recombinant human PDE4B2B enzyme expressed in yeast membranes[1]. |
| In vivo | GSK356278 (4 doses at 0.03, 0.1, 0.3, and 1.0 mg/kg for 6 weeks; p.o.) enhances performance in a nonhuman primate object retrieval test[1]. GSK356278 exhibits oral bioavailability (rat 91%, monkey 23%) and Cmax (rat 205, monkey 41 nM) following oral administration (rat 1, monkey 0.2 mg/kg). GSK356278 (0.1-0.1 mg/kg; p.o.) demonstrates efficacy in a nonhuman primate model of anxiety at exposures that do not induce emesis. GSK356278 (0.003-30 mg/kg; p.o.) shows anti-inflammatory activity in rodents at exposures that does not induce pica feeding[1]. |
| Alias | GSK-356278, GSK 356278 |
| Molecular Weight | 439.53 |
| Formula | C21H25N7O2S |
| Cas No. | 720704-34-7 |
| Smiles | CCn1ncc2c(NC3CCOCC3)c(cnc12)-c1nnc(Cc2sc(C)nc2C)o1 |
| Relative Density. | 1.50 g/cm3 (Predicted) |
Storage & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||
| Solubility Information | DMSO: 2 mg/mL (4.55 mM), Sonication is recommended. | ||||||||||
Solution Preparation Table | |||||||||||
DMSO
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Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
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(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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