P-glycoprotein (P-gp) also known as multidrug resistance protein 1 (MDR1) is an important protein of the cell membrane that pumps many foreign substances out of cells. More formally, it is an ATP-dependent efflux pump with broad substrate specificity. P-gp is extensively distributed and expressed in the intestinal epithelium where it pumps xenobiotics (such as toxins or drugs) back into the intestinal lumen, in liver cells where it pumps them into bile ducts, in the cells of the proximal tubular of the kidney where it pumps them into urine-conducting ducts, and in the capillary endothelial cells comprising the blood–brain barrier and blood-testis barrier, where it pumps them back into the capillaries. Some cancer cells also express large amounts of P-gp, which renders these cancers multi-drug resistant. P-gp is an ATP-dependent drug efflux pump for xenobiotic compounds with broad substrate specificity. It is responsible for decreased drug accumulation in multidrug-resistant cells and often mediates the development of resistance to anticancer drugs. This protein also functions as a transporter in the blood–brain barrier.
货号 | 产品名 | Cas | 产品描述 |
---|---|---|---|
PC11911 | Dofequidar fumarate | 153653-30-6 | MDR逆转剂,Dofequidar 延胡索酸盐(MS-209 延胡索酸盐)是口服活性的喹啉化合物,能抑制 ABCB1/P-gp,ABCC1/MDR-相关蛋白1。 |
PC12418 | Estradiol 17-(β-D-Glucuronide) (sodium salt) | 15087-02-2 | 多药耐药蛋白2(MRP2)的底物,Km: 75 μM,Estradiol 17-(β-D-Glucuronide) is a substrate of the multidrug resistance protein 2 (MRP2). |
PC12419 | Estradiol 3-(β-D-Glucuronide) (sodium salt) | 14982-12-8 | 多药耐药蛋白2(MRP2)的底物,β-estradiol 3-(β-d-glucuronide) (E23G) is a noncholestatic regioisomer of the estrogen metabolite, E217G (β-Estradiol 17-(β-d-glucuronide)) [1]. E23G functions as a substrate for multidrug resistance associated protein 2 (MRP2) [2]. |
PC12414 | Hypophyllanthin | 33676-00-5 | P-糖蛋白(P-gp)抑制剂,Hypophyllanthin 是 Phyllanthus spp 中主要的一种木质素,具有很强的抗炎活性。Hypophyllanthin 能直接抑制 P-gp 的活性,而不干扰 MRP2 活性。 |
PC12405 | Rhodamine 123 (chloride) | 62669-70-9 | 膜可渗透的阳离子染料,用作流出泵P-糖蛋白的底物,Rhodamine 123 是一种荧光染料(λex=503 nm, λem=527 nm)。 |
PC11885 | Tariquidar methanesulfonate, hydrate | 625375-83-9 | P-糖蛋白抑制剂,Tariquidar methanesulfonate, hydrate是有效和特异性的 P-glycoprotein (P-gp) 抑制剂,Kd值为5.1 nM。 |
PC11888 | Zosuquidar | 167354-41-8 | MDR调节剂,Zosuquidar (LY335979)是P-糖蛋白(P-gp)介导的多药抗性负调节剂,Ki为60 nM。 |