UCB7362
UCB7362 is an orally active and potent antimalarial plasmepsin X (PMX) inhibitor, with an IC50 of 7 nM. UCB7362 inhibits parasite growth.
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- Formule: C25H27Cl2N5O3
- Masse moléculaire:516.42
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Plasmodium |
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[1].
UCB7362 also demonstrates an improvement in selectivity against Cat D and Renin with an IC50 of 3889 nM and >10,000 nM, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
UCB7362 (IV (1 mg/kg), PO (10 mg/kg); once) shows moderate clearance in dog and cynomolgus monkey and moderate-high in rat[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Pf (Plasmodium falciparum) SCID mouse model[1]
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Dosage:10, 25 and 60 mg/kg
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Administration:Oral administration, twice a day, for 4 days, with the second administration 10 h after the first one
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Result:Cleared parasitemia from peripheral blood in a dose-dependent manner.
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Animal Model:Sprague Dawley rat[1]
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Dosage:1 mg/kg, 10 mg/kg
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Administration:IV (1 mg/kg), PO (10 mg/kg); once (Pharmacokinetic Analysis)
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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
Chemical Information
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Masse moléculaire 516.42
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Formule C25H27Cl2N5O3
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SMILES
O=C(NC1=CC=CC([C@@](CC(N2[C@@H]3C[C@H](C)OCC3)=O)(C)NC2=N)=C1Cl)C4=CC=CC(C#N)=C4.[H]Cl
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)