公告提醒:爱必信所有产品和服务仅用于科学研究,不用于临床应用及其他用途提供产品和服务(也不为任何个人提供产品和服务)! 抑制剂描述: 产品名称:Apremilast 产品别名:见爱必信官网 英文别名:Apremilast 靶点:PDE CAS:608141-41-9 纯度:>98% 外观:见爱必信官网 保存方法:Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution. 描述: Apremilast (CC-10004)是一种有效的PDE4和TNF-α抑制剂,IC50分别为74 nM和77 nM。Apremilast抑制PDE4比其他PDE家族的cAMP 或cGMP水解酶更有效。Apremilast作用于多种类型的细胞,具有广泛的抗炎活性,抑制TNF-α,IL-12和IL-23的产量,及NK和角质形成细胞的反应。Apremilast抑制IL-8中酵母多糖诱导的PMN产生,IC50为94 nM。 溶解性:DMSO :92 mg/mL (199.78 mM) 体外研究: Apremilast inhibits TNF-α release by lipopolysaccharide (LPS) with an IC50 of 104 nM (pIC50=6.98±0.2), which almost exactly replicates previous reported TNF-α inhibition by Apremilast on peripheral blood mononuclear cells (PBMCs) (IC50=110 nM) and which is similar to the potency of Apremilast for PDE4 enzymatic inhibition (IC50=74 nM). These results are clearly consistent with the hypothesis that Apremilast inhibits TNF-α by increasing intracellular cAMP levels. PKA, Epac1 and Epac2 knockdowns prevented TNF-α inhibition and IL-10 stimulation by Apremilast. 体内研究:Apremilast, orally administered (5 mg/kg), significantly inhibits TNF-α production in the air pouch by 39 % (61±6 % of vehicle, P . Apremilast is a novel, oral PDE4 inhibitor that has been shown to regulate inflammatory mediators. After oral administration of Apremilast, a mean maximum plasma concentration (Cmax) is found to be 67.00±14.87 ng/mL. The plasma concentration of Apremilast decreases rapidly and is eliminated from plasma with a terminal half-life of 0.92±0.46 h 产品信息订购:
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