| Description | iGOT1-01 is an effective inhibitor of glutamate oxaloacetate transaminase 1(GOT1) . iGOT1-01 has IC50s of 84.6 μM and 11.3 μM in GOT1/MDH1 assay and GOT1/GLOX/HRP assay, respectively. iGOT1-01 can be used in anti-cancer studies. |
| In vitro | iGOT1-01（3.125-200 μM；3小时）在PaTu8902胰腺癌细胞和DLD1结肠癌细胞中的两种细胞活性检测中显示出微弱至无毒性。在100 μM浓度下，iGOT1-01对MDH1的单独抑制活动未观察到[1]。 |
| In vivo | 在雌性CD1小鼠中，iGOT1-01（口服；20 mg/kg）表现出合理的生物利用度和暴露特性（t1/2=0.7小时，Cmax=4133 ng/mL，AUC(0-24小时)=11734小时ng/mL）[2]。 |
| Target activity | GOT1/MDH1:84.6 μM, GOT1/GLOX/HRP:11.3 μM |
| molecular weight | 320.39 |
| Molecular formula | C19H20N4O |
| CAS | 882256-55-5 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility | DMSO: 98 mg/mL (305.88 mM), Sonication is recommended. |
| References | 1. Melissa C Holt, et al. Biochemical Characterization and Structure-Based Mutational Analysis Provide Insight into the Binding and Mechanism of Action of Novel Aspartate Aminotransferase Inhibitors. Biochemistry. 2018 Nov 27;57(47):6604-6614. 2. Justin Anglin, et al. Discovery and optimization of aspartate aminotransferase 1 inhibitors to target redox balance in pancreatic ductal adenocarcinoma. Bioorg Med Chem Lett. 2018 Sep 1;28(16):2675-2678. |