
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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25MG | 983 | Get Quote |
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50MG | 1637 | Get Quote |
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100MG | 2682 | Get Quote |
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Biological Information
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Product NameApricitabine
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NoteResearch use only, not for human use.
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Brief DescriptionApricitabine (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) .
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DescriptionApricitabine (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.
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In VitroApricitabine (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.
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In VivoApricitabine (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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Synonyms——
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PathwayCell Cycle/DNA Damage
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TargetDNA/RNA Synthesis
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RecptorDNA/RNA Synthesis | HIV Protease
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Research Area——
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Indication——
Chemical Information
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CAS Number160707-69-7
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Formula Weight229.26
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Molecular FormulaC8H11N3O3S
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Purity>98% (HPLC)
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Solubility——
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SMILESO=C1N([C@@H]2S[C@H](CO)OC2)C=CC(N)=N1
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Chemical Name——
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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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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