| Description | Sucunamostat (SCO-792) hydrochloride is an orally active, reversible inhibitor of enteropeptidase, displaying inhibition constants (IC50) of 4.6 nM for rat enteropeptidase and 5.4 nM for human enteropeptidase. In vitro, it dissociates slowly from enteropeptidase, while in vivo, it hinders protein digestion [1]. |
| In vivo | Sucunamostat hydrochloride(10 和 30 mg/kg;口服,单次剂量)在实验中对大鼠经口摄入的蛋白质诱导血浆支链氨基酸(BCAA)水平上升表现出有效并且呈剂量依赖性的抑制作用[1]。在雄性Sprague-Dawley大鼠中,Sucunamostat hydrochloride的药代动力学参数显示,口服(PO)10 mg/kg与静脉注射(IV)2 mg/kg时,C max(ng/mL)分别为6.60 ± 1.36和564 ± 58,T max(h)为1.7 ± 0.6,AUC 0-24(ng/mL·h)为54.1 ± 7.5,AUC inf(ng/mL·h)为49.8 ± 5.4和304 ± 30,Vd SS(mL/kg)为1290 ± 299,CL p(mL/min/kg)为663 ± 66,生物利用度(%)为0.4。 |
| Synonyms | SCO-792 hydrochloride |
| molecular weight | 506.89 |
| Molecular formula | C22H23ClN4O8 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |