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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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 174391-92-5
- 分子式: C33H36N4O3
- 分子量:536.66
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
製品説明
IC50 & Target
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HIV-1 |
体外実験
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.
体内実験
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.
化学情報
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CAS 番号 174391-92-5
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分子量 536.66
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分子式 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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別名
DMP-450
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)