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Apremilast (CC-10004) 是一种口服有效的磷酸二酯酶 4 抑制剂,IC50为 74 nM。它抑制脂多糖释放TNF-α,IC50为 104 nM。
Apremilast (CC-10004) 是一种口服有效的磷酸二酯酶 4 抑制剂,IC50为 74 nM。它抑制脂多糖释放TNF-α,IC50为 104 nM。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 198 | 现货 | |
5 mg | ¥ 452 | 现货 | |
10 mg | ¥ 595 | 现货 | |
25 mg | ¥ 725 | 现货 | |
100 mg | ¥ 995 | 现货 | |
200 mg | ¥ 1,520 | 现货 | |
500 mg | ¥ 2,750 | 现货 |
产品描述 | Apremilast (CC-10004) (CC-10004) is a potent and orally active PDE4 (IC50=74 nM) with anti-inflammation activities. |
靶点活性 | PDE4:74 nM |
体外活性 | Apremilast通过抑制由脂多糖(LPS)引起的TNF-α释放,IC50为104 nM(pIC50=6.98±0.2),这一结果与之前报道的Apremilast对周围血单核细胞(PBMCs)的TNF-α抑制作用(IC50=110 nM)几乎完全一致,同时与Apremilast对PDE4酶抑制作用的效力相似(IC50=74 nM)。这些结果明确支持了Apremilast通过提高细胞内cAMP水平来抑制TNF-α的假设。PKA、Epac1和Epac2的敲除阻止了Apremilast对TNF-α的抑制和对IL-10的刺激[1]。 |
细胞实验 | 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]. |
别名 | 阿普斯特, 阿普司特, CC-10004 |
分子量 | 460.5 |
分子式 | C22H24N2O7S |
CAS No. | 608141-41-9 |
Smiles | [C@H](CS(C)(=O)=O)(N1C(=O)C=2C(C1=O)=CC=CC2NC(C)=O)C3=CC(OCC)=C(OC)C=C3 |
密度 | 1.381 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||
溶解度信息 | DMSO: 4.6 mg/mL (10 mM), Sonication is recommended. | ||||||||||||||||||||
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