Mozenavir dimethanesulfonate
Mozenavir dimethanesulfonate (DMP-450 dimethanesulfonate) is an orally active cyclic urea HIV-1 protease inhibitor with an IC50 of 76 nM. Mozenavir dimethanesulfonate 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 dimethanesulfonate is applicable to research related to HIV infection.
For research use only. We do not sell to patients.
- CAS No.: 177932-89-7
- Formula: C35H44N4O9S2
- Molecular Weight:728.88
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Storage:
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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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
HIV-1 |
In Vitro
Mozenavir (DMP-450) dimethanesulfonate 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 dimethanesulfonate 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 dimethanesulfonate 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.
Parmacokinetics
| Species | Dose | Route | CL | Vss | T1/2 | Cmax | Tmax | F |
|---|---|---|---|---|---|---|---|---|
| Rat[1] | 10 mg/kg | i.v. | 4.7 L/h/kg | 4.52 L/kg | 1.3 h | / | / | / |
| Rat[1] | 10 mg/kg | p.o. | / | / | / | 2.25 μM | 0.5 h | 70.5 % |
| Dog[1] | 10 mg/kg | i.v. | 0.21 L/h/kg | 1.35 L/kg | 3.6 h | / | / | / |
| Dog[1] | 10 mg/kg | p.o. | / | / | / | 11.19 μM | 2.0 h | 79.3 % |
| Rhesus monkey[1] | 10 mg/kg | i.v. | 1.20 L/h/kg | 1.37 L/kg | 0.8 h | / | / | / |
| Rhesus monkey[1] | 10 mg/kg | p.o. | / | / | / | 1.60 μM | 1.5 h | 25.7 % |
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 177932-89-7
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Molecular Weight 728.88
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Formula C35H44N4O9S2
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SMILES
CS(=O)(O)=O.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.CS(=O)(O)=O
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Synonyms
DMP-450 dimethanesulfonate
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Mozenavir dimethanesulfonate Related Classifications
HY-105148A Related Classifications
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