产品
编 号：F763021
分子式：C25H26ClN5O3
分子量：479.96
分子式：C25H26ClN5O3
分子量：479.96
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CAS No: 3031484-59-7
产品详情
生物活性：
UCB7362 is an orally active and potent antimalarial plasmepsin X (PMX) inhibitor, with an IC50 of 7 nM. UCB7362 inhibits parasite growth.
体内研究：
UCB7362 (10-60 mg/kg, Oral administration, twice a day, for 4 days) clears parasitemia from peripheral blood. UCB7362 (IV (1 mg/kg), PO (10 mg/kg); once) shows moderate clearance in dog and cynomolgus monkey and moderate-high in rat.Animal Model:Pf (Plasmodium falciparum) SCID mouse model
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
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.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)7931410
t1/2 (h)2.1
F (%)11
体外研究：
UCB7362 is substantially more potent against PMX than PMIX with an IC50 of 7 nM for the former compared to 142 nM for the latter. UCB7362 also demonstrates an improvement in selectivity against Cat D and Renin with an IC50 of 3889 nM and >10,000 nM, respectively.
UCB7362 is an orally active and potent antimalarial plasmepsin X (PMX) inhibitor, with an IC50 of 7 nM. UCB7362 inhibits parasite growth.
体内研究：
UCB7362 (10-60 mg/kg, Oral administration, twice a day, for 4 days) clears parasitemia from peripheral blood. UCB7362 (IV (1 mg/kg), PO (10 mg/kg); once) shows moderate clearance in dog and cynomolgus monkey and moderate-high in rat.Animal Model:Pf (Plasmodium falciparum) SCID mouse model
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
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.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)7931410
t1/2 (h)2.1
F (%)11
体外研究：
UCB7362 is substantially more potent against PMX than PMIX with an IC50 of 7 nM for the former compared to 142 nM for the latter. UCB7362 also demonstrates an improvement in selectivity against Cat D and Renin with an IC50 of 3889 nM and >10,000 nM, respectively.
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