| Description | INE963 demonstrates potent cellular activity against Pf 3D7 (EC50 = 6 nM) and achieves "artemisinin-like" kill kinetics in vitro with a parasite clearance time of <24 h. INE963 is also potent against P. falciparum and P. vivax clinical isolates from Brazil and Uganda with EC50’s ranging from 0.01 to 7.0 nM |
| In vitro | INE963对超过15种耐药Pf细胞系具有活性，其EC50值介于0.5-15 nM之间。INE963在体外对Pf 3D7的寄生虫减少比例日志值(log parasite reduction ratio)大于8.0，在无滞后阶段的条件下，10倍Pf 3D7 EC50剂量即可达到，且寄生虫清除时间(PCT99.9)小于24小时。INE963对於疟原虫相对于人类细胞的体外选择性，通过针对多种人类激酶生化测定的大约1000倍以上转变率得到体现[1]。 |
| In vivo | 在口服四次，每次30mg/kg INE963后，作为先导化合物的INE963在第五天所测得的寄生虫减少率显著，与未经治疗的对照小鼠相比减少了99.9%以上。此外，这些动物在治疗后的第60天没有显示出寄生虫复发的迹象，表明这些剂量达到了完全治愈的效果[1]。 |
| Target activity | Pf3D7:6 nM(EC50) |
| molecular weight | 402.51 |
| Molecular formula | C19H26N6O2S |
| CAS | 2640567-43-5 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility | DMSO: 50 mg/mL (124.22 mM) |
| References | 1. Taft BR, et, al. Discovery and Preclinical Pharmacology of INE963, a Potent and Fast-Acting Blood-Stage Antimalarial with a High Barrier to Resistance and Potential for Single-Dose Cures in Uncomplicated Malaria. J Med Chem. 2022 Mar 10;65(5):3798-3813. |