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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- 화학식: C25H27Cl2N5O3
- 분자량:516.42
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
All Parasite Isoforms
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Biological Activity
제품 설명
IC50 & Target
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Plasmodium |
In Vitro
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. Further protocols information, click here.
In Vivo
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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분자량 516.42
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화학식 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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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocol
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)