阿立他滨
- CAS号:160707-69-7
- 英文名:Apricitabine
- 中文名:阿立他滨
- CBNumber:CB41092857
- 分子式:C8H11N3O3S
- 分子量:229.26
- MOL File:160707-69-7.mol
- 沸点 :475.4±55.0 °C(Predicted)
- 密度 :1.73
- 溶解度 :DMSO: soluble
- 形态 :A solid
- 酸度系数(pKa) :13.83±0.10(Predicted)
阿立他滨性质、用途与生产工艺
- 生物活性 Apricitabine (SPD754; AVX754) 是 2'-脱氧-3'-oxa-4'-硫代胞苷 (dOTC) 的 (-) 对映体，是一种高度选择性和口服活性的 HIV-1 RT 逆转录酶抑制剂 (Ki=0.08 μM) 以及抑制 DNA 聚合酶 α, β 和 γ，Ki 值分别为 300 μM，12 μM 和 112.25 μM。Apricitabine (SPD754; AVX754) 表现出的好的抗逆转录病毒疗效，良好的耐受性，并且在初次抗逆转录病毒的 HIV 感染中耐药选择性的倾向较低。
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靶点
HIV-1
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体外研究
Apricitabine (SPD754; AVX754) is against clinical isolates of HIV-1 in cultured PBMCs with IC 50 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. Apricitabine (SPD754; AVX754) has antiviral activities agsinst HIV-1 clinical isolates resistant to nucleoside reverse transcriptase inhibitors in MT-4 cells, exhibits Mean IC 50 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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体内研究
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 T 1/2 , AUC 0–∞ , T max , C max 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 T 1/2 , AUC 0–∞ values of 12.7 mins, 226.9 μg/min/ml in female rats.
- 公司名称：CLEARSYNTH LABS LTD.
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- 国家：印度
- 产品数：6257
- 优势度：58
