| Description | Retrorsine selectively inhibits hepatocyte proliferation and following liver injury evokes small hepatocyte-like progenitor cells. Retrorsine can be used for the research of hepatocellular injury. |
| In vitro | Retrorsine 在 MDCK-hOCT1 细胞中抑制了 OCT1 介导的 1-甲基-4-苯基吡啶 (MPP(+)) 吸收，IC50 为 2.25±0.30μM [1]。Retrorsine (60 μM, 120 μM, 240 μM; 24小时) 显著降低了 HSEC-CYP3A4 细胞的活性和 GSH 水平，并增加了吡咯-蛋白质加合物的形成 [2]。 |
| In vivo | 在雄性Wistar大鼠中，Retrorsine（30 mg/kg；i.p.；两次）通过一个位于细胞周期G1/S过渡之前的阻滞，以及S或G2/M阶段的阻滞，损害了PBL模型中的肝脏再生[3]。 |
| Target activity | OCT1:2.2 μM |
| molecular weight | 351.39 |
| Molecular formula | C18H25NO6 |
| CAS | 480-54-6 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 95 mg/mL (270.35 mM), Sonication is recommended. |
| References | 1. Tu M, et al. Involvement of organic cation transporter 1 and CYP3A4 in retrorsine-induced toxicity. Toxicology. 2014 Aug 1;322:34-42. 2. Yao Lu, et al. Establishment of a novel CYP3A4-transduced human hepatic sinusoidal endothelial cell model and its application in screening hepatotoxicity of pyrrolizidine alkaloids. J Environ Sci Health C Toxicol Carcinog. 2020;38(2):169-185. 3. Christian Picard, et al. Retrorsine: a kinetic study of its influence on rat liver regeneration in the portal branch ligation model. J Hepatol. 2003 Jul;39(1):99-105. 4. F J Cubero, et al. Hepatic proliferation in Gunn rats transplanted with hepatocytes: effect of retrorsine and tri-iodothyronine. Cell Prolif. 2005 Jun;38(3):137-46. |