Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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.
パッケージサイズ | 在庫状況 | 単価(税別) | |||
---|---|---|---|---|---|
サンプルについてお問い合わせ | |||||
2 mg | 在庫あり | ¥ 8,000 | |||
5 mg | 在庫あり | ¥ 13,000 | |||
10 mg | 在庫あり | ¥ 20,500 | |||
25 mg | 在庫あり | ¥ 40,000 | |||
50 mg | 在庫あり | ¥ 74,000 | |||
100 mg | 在庫あり | ¥ 118,000 | |||
200 mg | 在庫あり | ¥ 160,500 | |||
500 mg | 在庫あり | ¥ 250,500 |
説明 | 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. |
ターゲット&IC50 | PDE4B:8.8 (pIC50), PDE4A:8.6 (pIC50), PDE4D:8.7 (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]. |
別名 | GSK-356278, GSK 356278 |
分子量 | 439.53 |
分子式 | C21H25N7O2S |
CAS No. | 720704-34-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 2 mg/mL (4.55 mM), Sonication is recommended.
You can also refer to dose conversion for different animals. 詳細
bottom
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.
GSK356278 720704-34-7 Metabolism PDE GSK-356278 anti-inflammatory Phosphodiesterase (PDE) GSK 356278 anxiolytic cognition Inhibitor phosphodiesterase PDE4 inhibit inhibitor