UCB7362 是一种口服有效的抗疟疾 (antimalarial) plasmepsin X (PMX) 抑制剂，其IC50为 7 nM。UCB7362 可抑制寄生虫 (parasite) 生长。
| 生物活性 | UCB7362 is an orally active and potentantimalarialplasmepsin X (PMX) inhibitor, with anIC50of 7 nM. UCB7362 inhibitsparasitegrowth[1]. |
| IC50& Target | |
体外研究
(In Vitro) | UCB7362 is substantially more potent against PMX than PMIX with an IC50of 7 nM for the former compared to 142 nM for the latter[1].
UCB7362 also demonstrates an improvement in selectivity against Cat D and Renin with an IC50of 3889 nM and >10,000 nM, respectively[1].
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体内研究
(In Vivo) | UCB7362 (10-60 mg/kg, Oral administration, twice a day, for 4 days) clears parasitemia from peripheral blood[1].
UCB7362 (IV (1 mg/kg), PO (10 mg/kg); once) shows moderate clearance in dog and cynomolgus monkey and moderate-high in rat[1].
| Animal Model: | Pf (Plasmodium falciparum) SCID mouse model[1] | | Dosage: | 10, 25 and 60 mg/kg | | Administration: | Oral administration, twice a day, for 4 days, with the second administration 10 h after the first one | | Result: | Cleared parasitemia from peripheral blood in a dose-dependent manner. |
| Animal Model: | Sprague Dawley rat[1] | | Dosage: | 1 mg/kg, 10 mg/kg | | Administration: | IV (1 mg/kg), PO (10 mg/kg); once (Pharmacokinetic Analysis) | | Result: | Pharmacokinetic Parameters of UCB7362 in Sprague-Dawley rats[1].
| IV (1 mg/kg) | PO (10 mg/kg) | | CL (mL/(min kg)) | 43.9 | | | Vss (L/kg) | 5.72 | | | Tmax(h) | | 3 | | Cmax(nM) | | 246 | | AUC0-24(nM*h) | 793 | 1410 | | t1/2(h) | 2.1 | | | F (%) | | 11 |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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