阿立他滨
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- CAS号:
- 160707-69-7
- 英文名:
- Apricitabine
- 英文别名:
- Avx754;Avx 754;Spd 754;CS-1026;(-)-dOTC;Bch 10618;APRICITABINE;(-)-Bch 10652;Unii-K1yx059ml1;Apricitabine [(-)-BCH10652
- 中文名:
- 阿立他滨
- 中文别名:
- 阿立他滨;阿普瑞西他滨;化合物 T14313;4-氨基-1-[(2R,4R)-2-(羟甲基)-1,3-氧硫杂环戊-4-基]-2(1H)-嘧啶酮
- CBNumber:
- CB41092857
- 分子式:
- C8H11N3O3S
- 分子量:
- 229.26
- MOL File:
- 160707-69-7.mol
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阿立他滨化学性质
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沸点:
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475.4±55.0 °C(Predicted)
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密度:
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1.73
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溶解度:
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DMSO: soluble
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形态:
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A solid
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酸度系数(pKa):
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13.83±0.10(Predicted)
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阿立他滨性质、用途与生产工艺
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。
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.
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.
阿立他滨
上下游产品信息
上游原料
下游产品
160707-69-7, 阿立他滨 相关搜索:
- 化合物 T14313
- 阿普瑞西他滨
- 阿立他滨
- 4-氨基-1-[(2R,4R)-2-(羟甲基)-1,3-氧硫杂环戊-4-基]-2(1H)-嘧啶酮
- 160707-69-7
- (-)-2'-Deoxy-3'-oxa-4'-thiocytidine
- 4-Amino-1-((2R,4R)-2-(hydroxymethyl)-1,3-oxathiolan-4-yl)pyrimidin-2(1H)-one
- CS-1026
- (-)-2'-Deoxy-3'-oxa-4'-thiocytidine (Apricitabine)
- Apricitabine (AVX754, SPD754)
- (-)-dOTC
- Apricitabine [(-)-BCH10652
- Unii-K1yx059ml1
- Spd 754
- Bch 10618
- Avx754
- Avx 754
- 2(1H)-Pyrimidinone, 4-amino-1-(2-(hydroxymethyl)-1,3-oxathiolan-4-yl)-, (2R-cis)-
- 2(1H)-Pyrimidinone, 4-amino-1-((2R,4R)-2-(hydroxymethyl)-1,3-oxathiolan-4-yl)-
- (-)-Bch 10652
- 4-Amino-1-[(2R,4R)-2-(hydroxymethyl)-1,3-oxathiolan-4-yl]-2(1H)-pyrimidinone
- APRICITABINE