产品
编 号:F758850
分子式:C9H7LiO4
分子量:186.09
产品类型
结构图
CAS No: 552-98-7
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产品详情
生物活性:
Aspirin (Acetylsalicylic Acid) lithium is an orally active, potent and irreversible inhibitor of cyclooxygenase COX-1 and COX-2, with IC50 values of 5 and 210 μg/mL, respectively. Aspirin lithium induces apoptosis. Aspirin lithium inhibits the activation of NF-κB. Aspirin lithium also inhibits platelet prostaglandin synthetase, and can prevent coronary artery and cerebrovascular thrombosis.
体内研究:
Aspirin lithium (5-150 mg/kg, PO, once) shows significant antipyretic activity in adult yeast-fevered male rats.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)
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.
体外研究:
Aspirin lithium inhibits COX-1 and COX-2 in human articular chondrocytes, with IC50 values of 3.57 μM and 29.3 μM, respectively.Aspirin lithium acetylates serine-530 of COX-1, thereby blocking thromboxane A synthesis in platelets and reducing platelet aggregation. Aspirin lithium 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. Aspirin lithium inhibits NF-κB-dependent transcription from the lgκ enhancer and the human immunodeficiency virus (HIV) long terminal repeat (LTR) in transfected T cells. Aspirin lithium induces apoptosis by the activation of caspases, the activation of p38 MAP kinase, release of mitochondrial cytochrome c, and activation of the ceramide pathway.