UCB7362
UCB7362 is an orally active and potent antimalarial plasmepsin X (PMX) inhibitor, with an IC50 of 7 nM. UCB7362 inhibits parasite growth.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Formel: C25H27Cl2N5O3
- Molecular Weight:516.42
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biologische Aktivität
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Chemical Information
- Protokoll
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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Biologische Aktivität
Beschreibung
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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Molecular Weight 516.42
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Formel 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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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Protokoll
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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.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
UCB7362 Related Classifications
HY-151568 Related Classifications
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