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Apricitabine

CAS No. 160707-69-7

Apricitabine( —— )

Catalog No. M33269 CAS No. 160707-69-7

Apricitabine (SPD754) is a highly selective and orally active HIV-1 reverse transcriptase inhibitor (Ki=0.08 μM), the (-) enantiomer of 2′-deoxy-3′-oxy-4′-thiocytidine (dOTC) .

Purity : >98% (HPLC)

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Biological Information

  • Product Name
    Apricitabine
  • Note
    Research use only, not for human use.
  • Brief Description
    Apricitabine (SPD754) is a highly selective and orally active HIV-1 reverse transcriptase inhibitor (Ki=0.08 μM), the (-) enantiomer of 2′-deoxy-3′-oxy-4′-thiocytidine (dOTC) .
  • Description
    Apricitabine (SPD754; AVX754), the (-) enantiomer of 2′-deoxy-3′-oxa-4′-thiocytidine (dOTC), is a highly selective and orally active HIV-1 reverse transcriptase (RT) inhibitor (Ki=0.08 μM), as well as inhibits DNA polymerases α, β, and γ with Ki value of 300 μM, 12 μM, and 112.25 μM, respectively. Apricitabine (SPD754; AVX754) shows promising antiretroviral efficacy, good tolerability and a low propensity for resistance selection in antiretroviral-naive HIV infection.
  • In Vitro
    Apricitabine (SPD754; AVX754) is against clinical isolates of HIV-1 in cultured?PBMCs with IC50?values of0.2 μM, 1.45 μM, 2.2 μM and 2.4?μM for HIV-1RF, Wild type, 3TC resistant, 3TC and AZT resistant, respectively.Apricitabine (SPD754; AVX754) has antiviral activities agsinstHIV-1 clinical isolates resistant to nucleoside reverse transcriptase inhibitors in MT-4 cells, exhibits Mean IC50 values of 20 μM, 25 μM, 30 μM,21 μM,55 μM,32 μM and 71 μM for HIV-1IIIB,Wild-type (control), Zidovudine-resistant, Lamivudine-resistant, Zidovudine-resistant/lamivudine-resistant, Abacavir-resistant and Stavudine-resistant viruses,respectively.
  • In Vivo
    Apricitabine (SPD754; AVX754) (oral adminstation; 10 mg/kg; once a day) exhibits a good oral bioavailability of 68% for males and 69.4% for females rats. And the T1/2, AUC0–∞, Tmax, Cmax are 62.2 mins, 157.4 μg/min/ml and 37.3 mins, 1.16 μg/ml in female rats.Apricitabine (SPD754; AVX754) (intravenous?injection; 10 mg/kg; once a day) exhibits the T1/2, AUC0–∞ values of 12.7 mins, 226.9 μg/min/ml in female rats.
  • Synonyms
    ——
  • Pathway
    Cell Cycle/DNA Damage
  • Target
    DNA/RNA Synthesis
  • Recptor
    DNA/RNA Synthesis | HIV Protease
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    160707-69-7
  • Formula Weight
    229.26
  • Molecular Formula
    C8H11N3O3S
  • Purity
    >98% (HPLC)
  • Solubility
    ——
  • SMILES
    O=C1N([C@@H]2S[C@H](CO)OC2)C=CC(N)=N1
  • Chemical Name
    ——

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. de Muys JM, et al. Anti-human immunodeficiency virus type 1 activity, intracellular metabolism, and pharmacokinetic evaluation of 2'-deoxy-3'-oxa-4'-thiocytidine.Antimicrob Agents Chemother. 1999 Aug;43(8):1835-44.?
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