1. Cell Cycle/DNA Damage
    Anti-infection
  2. Nucleoside Antimetabolite/Analog
    HIV
    DNA/RNA Synthesis
  3. Apricitabine

Apricitabine (Synonyms: SPD754; AVX754)

Cat. No.: HY-14913
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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[2].

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Apricitabine Chemical Structure

Apricitabine Chemical Structure

CAS No. : 160707-69-7

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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[1]. Apricitabine (SPD754; AVX754) shows promising antiretroviral efficacy, good tolerability and a low propensity for resistance selection in antiretroviral-naive HIV infection[2].

IC50 & Target[1]

HIV-1

 

In Vitro

Apricitabine (SPD754; AVX754) is against clinical isolates of HIV-1 in cultured PBMCs with IC50 values of 0.2 μM, 1.45 μM, 2.2 μM and 2.4 μM for HIV-1RF, Wild type, 3TC resistant, 3TC and AZT resistant, respectively[1].
Apricitabine (SPD754; AVX754) has antiviral activities agsinst HIV-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[2].

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[1].
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[1].

Clinical Trial
Molecular Weight

229.26

Formula

C₈H₁₁N₃O₃S

CAS No.

160707-69-7

SMILES

O=C1N=C(N)C=CN1[[email protected]@H]2S[[email protected]](CO)OC2

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Keywords:

ApricitabineSPD754AVX754SPD 754SPD-754AVX 754AVX-754Nucleoside Antimetabolite/AnalogHIVDNA/RNA SynthesisHuman immunodeficiency virusEnantiomerHIV-1antiretroviralvirus(-)dOTCinfectionMOLT-4DU-145HSFHT-1080HepG2Inhibitorinhibitorinhibit

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