阿立他滨
| 中文名称 | 阿立他滨 |
|---|---|
| 中文同义词 | 4-氨基-1-[(2R,4R)-2-(羟甲基)-1,3-氧硫杂环戊-4-基]-2(1H)-嘧啶酮;阿立他滨;阿普瑞西他滨;化合物 T14313 |
| 英文名称 | Apricitabine |
| 英文同义词 | APRICITABINE;4-Amino-1-[(2R,4R)-2-(hydroxymethyl)-1,3-oxathiolan-4-yl]-2(1H)-pyrimidinone;(-)-Bch 10652;2(1H)-Pyrimidinone, 4-amino-1-((2R,4R)-2-(hydroxymethyl)-1,3-oxathiolan-4-yl)-;2(1H)-Pyrimidinone, 4-amino-1-(2-(hydroxymethyl)-1,3-oxathiolan-4-yl)-, (2R-cis)-;Avx 754;Avx754;Bch 10618 |
| CAS号 | 160707-69-7 |
| 分子式 | C8H11N3O3S |
| 分子量 | 229.26 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 160707-69-7.mol |
| 结构式 |  |
阿立他滨 性质
| 沸点 | 475.4±55.0 °C(Predicted) |
|---|---|
| 密度 | 1.73 |
| 溶解度 | 可溶于DMSO |
| 形态 | 固体 |
| 酸度系数(pKa) | 13.83±0.10(Predicted) |
|
HIV-1
|
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.