Aspirin (Acetylsalicylic Acid) 是一种口服有效的不可逆的环氧合酶COX-1和COX-2抑制剂，IC50分别为 5 和 210 μg/mL. Aspirin 诱导细胞凋亡 (apoptosis)。Aspirin 可抑制NF-κB的活化。Aspirin 还抑制血小板前列腺素合成酶 (prostaglandin synthetase)，可预防冠状动脉和脑血管血栓形成。
| 生物活性 | Aspirin (Acetylsalicylic Acid) is an orally active, potent and irreversible inhibitor of cyclooxygenaseCOX-1andCOX-2, withIC50values of 5 and 210 μg/mL, respectively. Aspirin inducesapoptosis. Aspirin inhibits the activation ofNF-κB. Aspirin also inhibits plateletprostaglandin synthetase, and can prevent coronary artery and cerebrovascular thrombosis[1][2][3][4][5][6]. |
| IC50& Target[1] | COX-1 27.75 μM (IC50) | COX-2 1.17 mM (IC50) |
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体外研究
(In Vitro) | Aspirin inhibits COX-1 and COX-2 in human articular chondrocytes, with IC50values of 3.57 μM and 29.3 μM, respectively[2].
Aspirin acetylates serine-530 of COX-1, thereby blocking thromboxane A synthesis in platelets and reducing platelet aggregation[3].
Aspirin inhibits COX-2 protein expression through interference with binding of CCAAT/enhancer binding protein beta (C/EBPbeta) to its cognate site on COX-2 promoter/enhancer[3].
Aspirin inhibits NF-κB-dependent transcription from the lgκ enhancer and the human immunodeficiency virus (HIV) long terminal repeat (LTR) in transfected T cells[4].
Aspirin induces apoptosis by the activation of caspases, the activation of p38 MAP kinase, release of mitochondrial cytochrome c, and activation of the ceramide pathway[6].
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体内研究
(In Vivo) | Aspirin (5-150 mg/kg, PO, once) shows significant antipyretic activity in adult yeast-fevered male rats[7].
| Animal Model: | Male albino Charles River rats (200-250 g, 8 animals/group, fever was induced by 20 ml/kg of a 20 % aqueous suspension of brewer’s yeast which was injected SC in the back below the nape of the neck)[7] | | Dosage: | 5, 25, 50, 100 and 150 mg/kg | | Administration: | PO, once | | Result: | Produced a statistically significant decrease of 0.23 ℃ at 15 min post-drug at the dose of 150 mg/kg. Antipyretic effect gradually increased in magnitude until a peak effect of 1.96 ℃ was reached at 120 min post-drug. The ED50 of aspirin was found to be 10.3 mg/kg with confidence limits of 1.8-23.0 mg/kg. The antipyretic response to aspirin is dependent on the dose of the compound administered. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 400 mg/mL(2220.25 mM;Need ultrasonic) H2O : 0.1 mg/mL(0.56 mM;Need ultrasonic) 配制储备液 | 1 mM | 5.5506 mL | 27.7531 mL | 55.5062 mL | | 5 mM | 1.1101 mL | 5.5506 mL | 11.1012 mL | | 10 mM | 0.5551 mL | 2.7753 mL | 5.5506 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 10 mg/mL (55.51 mM); Clear solution
此方案可获得 ≥ 10 mg/mL (55.51 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 100.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 10 mg/mL (55.51 mM); Clear solution
此方案可获得 ≥ 10 mg/mL (55.51 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 100.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 3. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 10 mg/mL (55.51 mM); Clear solution
此方案可获得 ≥ 10 mg/mL (55.51 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 100.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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