160707-69-7
160707-69-7 結(jié)構(gòu)式
基本信息
阿普瑞西他濱
4-氨基-1-[(2R,4R)-2-(羥甲基)-1,3-氧硫雜環(huán)戊-4-基]-2(1H)-嘧啶酮
CS-1026
Avx 754
Spd 754
Bch 10618
APRICITABINE
(-)-Bch 10652
Unii-K1yx059ml1
(-)-2'-Deoxy-3'-oxa-4'-thiocytidine (Apricitabine)
4-Amino-1-((2R,4R)-2-(hydroxymethyl)-1,3-oxathiolan-4-yl)pyrimidin-2(1H)-one
常見問題列表
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HIV-1
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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.