| Description | CP-100356 hydrochloride is an orally active and low micromolar dual inhibitor of MDR1 (P-gp) and BCRP, a nucleotide-derived substrate analogue with inhibitory effects on MDR1-mediated Calcein-AM transporter and BCRP-mediated Prazosin transporter.CP-100356 Inhibits OATP1B1, induces stomatal opening in the dark. |
| In vitro | 在人源 MDR1 转染MDCKII细胞中，CP-100356 hydrochloride 抑制了乙酰甲氧基荧光素(calcein-AM)的摄取(IC50约为0.5 +/- 0.07microM)和地高辛的转运(IC50约为1.2 +/- 0.1microM)。CP-100356 hydrochloride 对人 BCRP 转染 MDCKII 细胞中的普拉索辛转运的抑制(IC50约为1.5 +/- 0.3 microM)证实了其双重 MDR1/BCRP 抑制性质[1]。 |
| In vivo | 在大鼠中，与 MDR1 底物非索非丁和双重 MDR1/BCRP 底物普拉索辛共同给药后，检查了 CP-100356 hydrochloride 的体内抑制效应。与增加剂量的 CP-100356 hydrochloride 共同给药导致非索非丁的系统暴露量显著增加(在24 mg/kg的 CP-100356 hydrochloride 剂量下，C(max)和AUC增加了36倍和80倍)。在 CP-100356 hydrochloride 预处理的大鼠中，普拉索辛的药代动力学也显示出显著差异，其AUC增加了2.6倍[1]。[1]。 |
| Target activity | MDR1:0.5 µM, BCRP:1.5 µM (in MDCKII cells) |
| Synonyms | CP-100356 HCl, CP 100356 hydrochloride |
| molecular weight | 597.1 |
| Molecular formula | C31H37ClN4O6 |
| CAS | 142715-48-8 |
| Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 5 mg/mL (8.37 mM), Sonication is recommended. |
| References | 1. Kalgutkar AS,et al. N-(3,4-dimethoxyphenethyl)-4-(6,7-dimethoxy-3,4-dihydroisoquinolin-2[1H]-yl)-6,7-dimethoxyquinazolin-2-amine (CP-100,356) as a "chemical knock-out equivalent" to assess the impact of efflux transporters on oral drug absorption in the rat. J Pharm Sci. 2009 Dec;98(12):4914-27. |