Apricitabine
Based on 1 Customer Validation
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.
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- 純度: 99.8%
- CAS 番号: 160707-69-7
- 分子式: C8H11N3O3S
- 分子量:229.26
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保管条件:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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生物活性
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HIV-1 |
DNA Polymerase |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| T-cell | EC50 |
1 μM
Compound: Apricitabine, ATC
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Antiviral activity against HIV in T cells assessed as inhibition of viral replication
Antiviral activity against HIV in T cells assessed as inhibition of viral replication
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[PMID: 17517847] |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 160707-69-7
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性状 Solid
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分子量 229.26
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分子式 C8H11N3O3S
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Color White to off-white
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SMILES
O=C1N=C(N)C=CN1[C@@H]2S[C@H](CO)OC2
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別名
SPD754; AVX754
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
純度とドキュメンテーション
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データシート (272 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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取扱説明書 (2659 KB)
参考文献
[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. [Content Brief]
[2]. Cahn P, et al. Efficacy and tolerability of 10-day monotherapy with apricitabine in antiretroviral-naive, HIV-infected patients.AIDS. 2006 Jun 12;20(9):1261-8. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Apricitabine 関連分類
HY-14913 関連分類
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