货号 | 产品名 | 中文名称 | 产品描述 |
---|---|---|---|
SJ-MX0480 | Anacetrapib (MK-0859) | 安塞曲匹 |
Anacetrapib (MK-0859)是一种有效的和选择性的胆固醇酯转运蛋白(CETP)抑制剂,强烈抑制CETP介导的胆固醇酯和甘油酸三脂转运,IC50值分别为16 nM和29 nM。Anacetrapib 作用于 rhCETP 和突变CETP(C13S),IC50 分别为 7.9±2.5 nM 和 11.8±1.9 nM。Anacetrapib可强效降低低密度脂蛋白(LDL)胆固醇水平和增加高密度脂蛋白(HDL)胆固醇水平,且无任何副作用,目前被用来治疗原发性高胆固醇血症和混合性高脂血症。 |
SJ-MX2412 | Evacetrapib | Evacetrapib 是一种有效的选择性的 CETP 抑制剂,在人血浆中,抑制人重组 CETP 蛋白 (IC50 为 5.5 nM) 和 CETP 活性,IC50 为 36 nM。 | |
SJ-MX3264 | Dalcetrapib | 达塞曲匹 | Dalcetrapib is a potent CETP modulator. It is a thioester pro-drug that is rapidly hydrolyzed to generate a pharmacologically active thiol. Dalcetrapib modulates cholesteryl ester transfer protein (CETP) activity to raise high-density lipoprotein cholesterol (HDL-C). It achieves 50% inhibition of CETP activity in human plasma at a concentration of 9 μM. |
SJ-MX4553 | Torcetrapib | Torcetrapib is a cholesteryl ester transfer protein (CETP) inhibitor; a drug being developed to treat hypercholesterolemia (elevated cholesterol levels) and prevent cardiovascular disease. |