Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Apremilast (CC-10004) (CC-10004) is a potent and orally active PDE4 (IC50=74 nM) with anti-inflammation activities.
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 | |||||
5 mg | 在庫あり | ¥ 10,000 | |||
10 mg | 在庫あり | ¥ 13,500 | |||
25 mg | 在庫あり | ¥ 16,500 | |||
100 mg | 在庫あり | ¥ 22,500 | |||
200 mg | 在庫あり | ¥ 36,500 | |||
500 mg | 在庫あり | ¥ 61,000 | |||
1 mL * 10 mM (in DMSO) | 在庫あり | ¥ 11,000 |
説明 | Apremilast (CC-10004) (CC-10004) is a potent and orally active PDE4 (IC50=74 nM) with anti-inflammation activities. |
ターゲット&IC50 | PDE4:74 nM |
In vitro | Apremilast inhibits TNF-α release by lipopolysaccharide (LPS) with an IC50 of 104 nM (pIC50=6.98±0.2), which almost exactly replicates previous reported TNF-α inhibition by Apremilast on peripheral blood mononuclear cells (PBMCs) (IC50=110 nM) and which is similar to the potency of Apremilast for PDE4 enzymatic inhibition (IC50=74 nM). These results are clearly consistent with the hypothesis that Apremilast inhibits TNF-α by increasing intracellular cAMP levels. PKA, Epac1 and Epac2 knockdowns prevented TNF-α inhibition and IL-10 stimulation by Apremilast[1]. |
細胞研究 | Apremilast is solubilized in DMSO and stored, and then diluted with appropriate media (DMSO 0.025%) before use[1]. Raw 264.7 cells (100,000) are grown in 96-well plates. After 24 h, cells are stimulated with vehicle (final concentration of 0.025% DMSO) or with Apremilast at the indicated concentrations. After 30 minutes cells are stimulated with LPS 1 μg/mL for 4 h. When studying CGS21680 , SCH58261, ZM241385, BAY60-6583, or GS6201, the adenosine receptor ligands are added 15 minutes before Apremilast. Methotrexate is added 24 h and 1 h before Apremilast. Supernates are then collected and TNF-α levels are quantified with the Mouse TNF-α Quantikine ELISA Kit. IC50 (EC50) calculations are made using non-linear regression, sigmoidal dose-response, constraining the top to 100 % and bottom to 0 %, allowing variable slope, using GraphPad Prism v6.00[1]. |
別名 | CC-10004 |
分子量 | 460.5 |
分子式 | C22H24N2O7S |
CAS No. | 608141-41-9 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 4.6 mg/mL (10 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.
Apremilast 608141-41-9 Apoptosis Metabolism TNF PDE TNFR orally TNF Receptor nucleotide inhibit lipopolysaccharide LPS phosphodiesterase CC 10004 PBMC Tumor Necrosis Factor Receptor CC10004 cyclic Phosphodiesterase (PDE) available CC-10004 Inhibitor type-4 inhibitor