Apricitabine

Research use only, not for human use.

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) .

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.

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.

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.

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Cell Cycle/DNA Damage

DNA/RNA Synthesis

DNA/RNA Synthesis | HIV Protease

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160707-69-7

229.26

C8H11N3O3S

>98% (HPLC)

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O=C1N([C@@H]2S[C@H](CO)OC2)C=CC(N)=N1

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(-20℃)

With Ice Pack

≥ 2 years