货号 | 17631-1mg |
描述 | Secreted phospholipases A2(sPLA2s) are a diverse family of low molecular weight PLA2s with tissue-specific expression patterns and actions.1 The group IIA sPLA2(sPLA2-IIA) was originally purified from platelets and exudates from patients with rheumatoid arthritis.1 Its expression can be induced by inflammatory mediators, and mouse studies suggest that it may play roles in colorectal polyposis, atherosclerosis, and bacterial infections.1,2 YM-26734 is a derivative of a compound isolated from the fruit of H. amygdaline that competitively inhibits rabbit platelet sPLA2 with an IC50 value of 85 nM.3 It inhibits sPLA2-hGIIA, -mGIIA, -rGIIA, -hGV, -mGV, -hGX, and -mGX with IC50 values of 80, 30, 120, 110, 520, >1600, and >1600 nM, respectively.4,5 YM-26734 displays minimal activity at cytosolic PLA2, COX and lipoxygenase.3 At 45 µg/ear or 11 mg/kg i.v., YM-26734 has been used to ameliorate local inflammatory responses in TPA-induced mouse ear edema.3 |
供应商 | Cayman |
应用文献 | |
1.Murakami, M.,Taketomi, Y.,Miki, Y., et al. Recent progress in phospholipase A2 research: From cells to animals to humans. Progress in Lipid Research 50(2), 152-192 (2011). 2.Murakami, M.,Taketomi, Y.,Girard, C., et al. Emerging roles of secreted phospholipase A2 enzymes: Lessons from transgenic and knockout mice. Biochimie 92(6), 561-582 (2010). 3.Miyake, A.,Yamamoto, H.,Kubota, E., et al. Suppression of inflammatory responses to 12-O-tetradecanoyl-phorbol-13-acetate and carrageenin by YM-26734, a selective inhibitor of extracellular group II phospholipase A2. British Journal of Pharmacology 110, 447-453 (1993). 4.Oslund, R.C.,Cermak, N.,Verlinde, C.L.M.J., et al. Simplified YM-26734 inhibitors of secreted phospholipase A2 group IIA. Bioorganic & Medicinal Chemistry Letters 18(20), 5415-5419 (2008). 5.Lambeau, G., and Gelb, M.H. Biochemistry and physiology of mammalian secreted phospholipases A2. Annual Reviews of Biochemistry 77, 495-520 (2008). | |
运输条件 | Room temperature in continental US; may vary elsewhere |
存放说明 | -20 |
纯度 | ≥95% |
计算分子量 | 731 |
分子式 | C45H62O8 |
CAS号 | 144337-18-8 |
稳定性 | ≥ 2 years |
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