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Aspirin (Acetylsalicylic Acid) 是一种 COX 抑制剂,抑制 COX1 和 COX2 (IC50=5/210 μg/mL),具有选择性、不可逆性和口服活性。Aspirin 也是一种组蛋白去乙酰化酶抑制剂,可上调细胞周期阻滞蛋白 p21。Aspirin 具有抗炎、解热镇痛、抗血小板聚集能多种活性。
Aspirin (Acetylsalicylic Acid) 是一种 COX 抑制剂,抑制 COX1 和 COX2 (IC50=5/210 μg/mL),具有选择性、不可逆性和口服活性。Aspirin 也是一种组蛋白去乙酰化酶抑制剂,可上调细胞周期阻滞蛋白 p21。Aspirin 具有抗炎、解热镇痛、抗血小板聚集能多种活性。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
500 mg | ¥ 333 | 现货 | |
1 g | ¥ 418 | 现货 | |
5 g | ¥ 671 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 418 | 现货 |
产品描述 | Aspirin (Acetylsalicylic Acid) is a COX inhibitor that inhibits COX1 and COX2 (IC50=5/210 μg/mL) with selective, irreversible, and oral activity. Aspirin is also a histone deacetylase inhibitor that up-regulates the cell cycle blocking protein, p21. Aspirin has a variety of activities. Aspirin has anti-inflammatory, antipyretic and analgesic, and antiplatelet aggregation activities. |
靶点活性 | COX-2:210 μg/mL, COX-1:5μg/mL |
体外活性 | 方法: 结直肠癌细胞 SW620、LoVo、RKO 和 DLD-1 用 Aspirin (2 mM) 和 Cisplatin (5-80 µM) 处理 48 h,使用 MTT assay 检测细胞活力。 结果: 联合用药更有效地降低了结肠癌细胞的生存能力。联合治疗导致 Cisplatin 的 IC50 值显著降低。[1] 方法: 成骨细胞 MG-63 用 Aspirin (1-1000 µM) 处理 24 h,使用 Flow cytometry 检测细胞周期。 结果: 1、10、20 µM 剂量的 Aspirin 治疗 24 h 后,对 MG-63 细胞周期无明显影响。然而,在 100 和 1000 µM 的剂量下,G0/G1 期的细胞百分比显著增加。[2] |
体内活性 | 方法: 为检测体内抗肿瘤活性,将 Aspirin (100 mg/kg,灌胃给药,每天一次) 和 Cisplatin (3 mg/kg,腹腔注射,每三天一次) 给药给携带 LoVo 异种移植物的裸鼠,持续 18 天。 结果: Aspirin 与 Cisplatin 协同抑制结肠癌裸鼠移植瘤生长,并且这些作用至少部分通过调节 PI3K-Akt、RAF-MEK-ERK 和 NF-κB/COX-2 信号通路发挥。[1] |
细胞实验 | Chondrocytes are isolated from articular cartilage of donors with no articular disease. Unstimulated and interleukin 1 (IL-1) stimulated chondrocytes are used as models to study the effects of drugs on COX-1 and COX-2. Cells are incubated with vehicle or drugs (Asprin); supernatants are removed and the level of prostaglandin E2 (PGE2) in each sample is determined by enzyme immunoassay. IC50s are calculated from the reduction in PGE2 content by different concentrations of the test substance by linear regression analysis[5]. |
别名 | Acetylsalicylate, Acetylsalicylic Acid, 阿司匹林, 邻乙酰水杨酸, ASA |
分子量 | 180.16 |
分子式 | C9H8O4 |
CAS No. | 50-78-2 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||||||||||||
溶解度信息 | 10% DMSO+90% Saline: 1.8 mg/mL (9.99 mM), Please add co-solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. H2O: 1.80 mg/mL (10 mM), Sonication and heating are recommended. DMSO: 50 mg/mL (277.53 mM) | |||||||||||||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||||||||||||
10% DMSO+90% Saline/H2O/DMSO
H2O/DMSO
DMSO
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