产品说明书

Zalcitabine

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Chemical Structure| 7481-89-2 同义名 : 扎西他滨 ;2',3'-Dideoxycytidine;ddC;dideoxycytidine, Brand name: Hivid.;2′-3′-dideoxycytidine;2’,3’-Dideoxycytidine;Ro 24-2027/000;NSC 606170;Dideoxycytidine
CAS号 : 7481-89-2
货号 : A310205
分子式 : C9H13N3O3
纯度 : 98%
分子量 : 211.218
MDL号 : MFCD00012188
存储条件：

粉末 Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 60 mg/mL(284.07 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 25 mg/mL(118.36 mM)
动物实验配方：

PO 0.5% CMC-Na 30 mg/mL clear

生物活性
描述 Zalcitabine is a potent nucleoside analogue reverse transcriptase inhibitor used in the treatment of HIV infection. Zalcitabine is a dideoxynucleoside antiretroviral agent that is phosphorylated to the active metabolite 2',3'-dideoxycytidine 5'-triphosphate (ddCTP) within both uninfected and HIV-infected cells. At therapeutic concentrations, ddCTP inhibits HIV replication by inhibiting the enzyme reverse transcriptase and terminating elongation of the proviral DNA chain[3]. Zalcitabine exhibits the inhibition effect on the cellular uptake of [3H]-PAH in CHO/hOAT1 cells with an IC50 value of 1.23 mM. Furthermore, the cellular uptake of zalcitabine increased threefold with the enhancement of hOATI activity in CHO/hOAT1 cells[4].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

4.73mL

0.95mL

0.47mL

23.67mL

4.73mL

2.37mL

47.34mL

9.47mL

4.73mL
参考文献

[1]Jin MJ, Han HK. Interaction of zalcitabine with human organic anion transporter 1. Pharmazie. 2006 May;61(5):491-2.

[2]Yarchoan R, Klecker RW, et al. Administration of 3'-azido-3'-deoxythymidine, an inhibitor of HTLV-III/LAV replication, to patients with AIDS or AIDS-related complex. Lancet. 1986 Mar 15;1(8481):575-80.

[3]Adkins JC, Peters DH, Faulds D. Zalcitabine. An update of its pharmacodynamic and pharmacokinetic properties and clinical efficacy in the management of HIV infection. Drugs. 1997;53(6):1054-1080.

[4]Jin MJ, Han HK. Interaction of zalcitabine with human organic anion transporter 1. Pharmazie. 2006;61(5):491-492.