Abacavir

- Overview
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    Background
    
    IC50 Value: 0.26 microM for HIV-1[1] Abacavir,(-)-(1S,4R)-4-[2-amino-6-(cyclopropylamino)-9H-purin-9-yl]-2-cyclopentene-1-methanol, is a novel purine carbocyclic nucleoside analogue that has been approved by the FDA for the treatment of HIV (as Ziagen trade mark [abacavir sulfate]) [2]. in vitro: In erythrocytes, abacavir influx was rapid, nonsaturable (rate constant=200 pmol/s/mM/microl cell water), and unaffected by inhibitors of nucleoside or nucleobase transport[2]. in vivo: pharmacokinetic, distribution, and toxicological profiles of 1592U89 were distinct from and improved over those of CBV, probably because CBV itself was not appreciably formed from 1592U89 in cells or animals (<2%). The 5'-triphosphate of CBV was a potent, selective inhibitor of HIV-1 RT, with Ki values for DNA polymerases (alpha, beta, gamma, and epsilon which were 90-, 2,900-, 1,200-, and 1,900-fold greater, respectively, than for RT (Ki, 21 nM). 1592U89 was relatively nontoxic to human bone marrow progenitors erythroid burst-forming unit and granulocyte-macrophage CFU (IC50s, 110 microM) and human leukemic and liver tumor cell lines[1]. Clinical trial: Estimate The Effect Of Lersivirine On The Pharmacokinetics Of Abacavir + Lamivudine In Healthy Subjects. Phage1
- Properties
  - Alternative Name
    
    Ziagen; [(1S,4R)-4-[2-amino-6-(cyclopropylamino)purin-9-yl]cyclopent-2-en-1-yl]methanol
    
    CAS Number
    
    136470-78-5
    
    Molecular Formula
    
    C14H18N6O
    
    Molecular Weight
    
    286.33
    
    Appearance
    
    A solid
    
    Purity
    
    98.00%
    
    Solubility
    
    ≥39.3 mg/mL in EtOH with gentle warming; ≥57 mg/mL in DMSO; ≥7.16 mg/mL in H2O
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only

Abacavir

Background

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