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87190-79-2

中文名稱 3'-疊氮基-2',3'-二脫氧-5-甲基胞苷
英文名稱 3'-azido-2',3'-dideoxy-5-methylcytidine
CAS 87190-79-2
分子式 C10H14N6O3
分子量 266.26
MOL 文件 87190-79-2.mol
更新日期 2023/03/20 15:41:21
87190-79-2 結(jié)構(gòu)式 87190-79-2 結(jié)構(gòu)式

基本信息

中文別名
3'-疊氮基-2',3'-二脫氧-5-甲基胞苷
英文別名
CS-92
AzddMeC
3'-azido-2',3'-dideoxy-5-methylcytidine
3'-Azido-2',3'-dideoxy-4-deoxo-4-imino-5-methyluridine

物理化學(xué)性質(zhì)

儲存條件4°C, away from moisture
溶解度DMSO : 200 mg/mL (751.15 mM; Need ultrasonic)
形態(tài)Solid
顏色White to off-white

常見問題列表

生物活性
AzddMeC (CS-92) 是一種抗病毒核苷類似物,也是一種有效的,選擇性的,具有口服活性的 HIV-1 逆轉(zhuǎn)錄酶和 HIV-1 復(fù)制的抑制劑。在感染 HIV-1 的人類 PBM 細(xì)胞和感染 HIV-1 的人類巨噬細(xì)胞中,AzddMeC 的 EC50 值分別為 9 nM 和 6 nM。
靶點(diǎn)

HIV-1

9 nM (EC 50 , Human PBM cells)

HIV-1

6 nM (EC 50 , Human macrophages)

體外研究

AzddMeC (CS-92) is also effective against HIV-2 in lymphocytes. The replication of Friend murine virus is only weakly inhibited, and no effect is observed against HSV type 1 and type 2 and coxsackievirus B4. The interaction of the 5'-triphosphate of AzddMeC with HIV-1 reverse transcriptase indicated competitive inhibition (the inhibition constant, Kis, is 9.3 nM).

體內(nèi)研究

The pharmacokinetics of AzddMeC are characterized following intravenous and oral administration of 60 mg/kg of the compound to male rhesus monkeys. 3'-azido-3'-deoxythymidine (AZT) is a major metabolite of AzddMeC in monkeys. AzddMeC concentrations in serum declined rapidly in a biexponential fashion with the terminal half-life ranging from 0.5 to 1.3 hr. Renal excretion of unchanged nucleoside and metabolic deamination yielding AZT are the primary routes of AzddMeC clearance. The oral bioavailability is 26%.

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