Mozenavir
Mozenavir (DMP-450) is an orally active cyclic urea HIV-1 protease inhibitor with an IC50 of 76 nM. Mozenavir inhibits replication by targeting viral protease, blocks viral polyprotein processing, and induces the production of core-uncondensed, immature, non-infectious viral particles in chronically infected cells. Mozenavir is applicable to research related to HIV infection.
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- CAS No.: 174391-92-5
- Formule: C33H36N4O3
- Masse moléculaire:536.66
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Activité biologique
Description
IC50 & Target
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HIV-1 |
In Vitro
Mozenavir (DMP-450) potently and selectively inhibits purified HIV-1 protease, with a Ki of 0.28 nM against peptide substrates and an IC50 of 76 nM against Gag polyprotein substrates[1].
Mozenavir potently inhibits the replication of wild-type and mutant HIV strains in MT-2, Molt-4, PBMC and U937 cells, with a mean IC90 of 144 nM. It also induces the production of immature viral particles, and exhibits low cytotoxicity in MT-2 cells (TC50 > 80 μM)[1].
Mozenavir shows reduced potency against single-mutant HIV strains (with a 2.8- to 7-fold increase in IC90), and significantly reduced potency against double-mutant and in vitro-selected multi-mutant HIV strains (with a maximum 100-fold increase in IC90)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Balb C (female, 30 days old)[1]
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Dosage:10 μg (i.m.); 100 mg/kg (p.o.)
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Administration:i.m.; single dose per quadriceps muscle
p.o.; twice daily; 2 days -
Result:Achieved luciferase activity of 74,183 light units per mg of muscle extract, matching activity seen with luciferase plasmid alone.
Achieved luciferase activity of 74,863 light units per mg of muscle extract, matching activity seen with luciferase plasmid alone.
Chemical Information
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CAS No. 174391-92-5
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Masse moléculaire 536.66
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Formule C33H36N4O3
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SMILES
O[C@H]([C@H]([C@H](N(C1=O)CC2=CC(N)=CC=C2)CC3=CC=CC=C3)O)[C@@H](CC4=CC=CC=C4)N1CC5=CC(N)=CC=C5
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Synonyms
DMP-450
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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)