化合物 T14313_化工百科

中文名	阿立他滨
英文名	Apricitabine
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
英文别名	Avx 754 CS-1026 Apricitabine APRICITABINE (-)-Bch 10652 4-Amino-1-((2R,4R)-2-(hydroxymethyl)-1,3-oxathiolan-4-yl)pyrimidin-2(1H)-one 4-Amino-1-[(2R,4R)-2-(hydroxymethyl)-1,3-oxathiolan-4-yl]-2(1H)-pyrimidinone 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)-
CAS	160707-69-7
化学式	C8H11N3O3S
分子量	229.26
InChI	InChI=1/C8H11N3O3S/c9-5-1-2-11(8(13)10-5)6-4-14-7(3-12)15-6/h1-2,6-7,12H,3-4H2,(H2,9,10,13)/t6-,7-/m1/s1
密度	1.73
沸点	475.4±55.0 °C(Predicted)
酸度系数	13.83±0.10(Predicted)
存储条件	Room Temprature
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.
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) (intravenousinjection; 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.