Darunavir

- Overview
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    Background
    
    Darunavir is an orally-bioavailable non-peptidic inhibitor of human immunodeficiency virus type 1 (HIV-1) protease that selectively inhibits HIV-1 protease enzyme induced cleavage of gag and gag-pol poly-proteins preventing the maturation of virions and also inhibits the dimerization of HIV-1 protease suppressing proteolytic activity and subsequent replication of HIV-1. Study results have shown that darunavir exhibits potent inhibition against HIV-1 with a value of 50% inhibition concentration IC50 of 0.003 μmol/L in HIV-1 infected MT-2 cells. Darunavir binds to HIV-1 protease with considerably high affinity and fits closely with the substrate envelop leading to its potent ability to inhibit multidrug-resistant HIV strains.
- Properties
  - Alternative Name
    
    (E)-(3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl hydrogen ((2S,3R)-4-(4-amino-N-isobutylphenylsulfonamido)-3-hydroxy-1-phenylbutan-2-yl)carbonimidate
    
    CAS Number
    
    206361-99-1
    
    Molecular Formula
    
    C27H37N3O7S
    
    Molecular Weight
    
    547.66
    
    Appearance
    
    A solid
    
    Purity
    
    99.53%
    
    Solubility
    
    ≥22.65 mg/mL in DMSO; insoluble in H2O; ≥4.94 mg/mL in EtOH with ultrasonic
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. Velichkovska M, Surnar B, et al. "Targeted Mitochondrial COQ(10) Delivery Attenuates Antiretroviral-Drug-Induced Senescence of Neural Progenitor Cells." Mol Pharm. 2019 Feb 4;16(2):724-736. PMID:30592424
    2. Lan, Jie, et al. "Provirus Activation Plus CD59 Blockage Triggers Antibody-Dependent Complement-Mediated Lysis of Latently HIV-1–Infected Cells." The Journal of Immunology (2014): 1303030. PMID:25149467

Darunavir

Background

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