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| 产地 | 国产 |
| 品牌 | Solarbio |
| 货号 | IA0850 |
| 用途 | |
| 包装规格 | 20mg 10mM*1mL in DMSO 50mg |
| CAS编号 | 59277-89-3 |
| 纯度 | 98% |
| 是否进口 | 否 |
| CAS | 59277-89-3 |
| 中文名称 | 阿昔洛韦 |
| 英文名称 | Acyclovir |
| 别名 | 阿昔洛维;Zovir |
| 纯度 | HPLC≥98% |
| 分子式 | C8H11N5O3 |
| 分子量 | 225.2 |
| 外观（性状） | White to off-white Solid |
| 储存条件 | Powder : 2-8℃, 2 years; In solvent(母液): -20℃, 1 month; -80℃, 6 months |
| 溶解性 | Soluble in DMSO ≥2mg/mL(Need ultrasonic) |
| MDL | MFCD00057880 |
| EC | EINECS 261-685-1 |
| InChIKey | MKUXAQIIEYXACX-UHFFFAOYSA-N |
| InChI | InChI=1S/C8H11N5O3/c9-8-11-6-5(7(15)12-8)10-3-13(6)4-16-2-1-14/h3,14H,1-2,4H2,(H3,9,11,12,15) |
| PubChem CID | 135398513 |
| SMILES | O=C1NC(N)=NC2=C1N=CN2COCCO |
| 描述 | (It is a class of thymidine kinase that can inhibit the herpes virus.) |
| 靶点 | HSV |
| 通路 | Anti-infection |
| 生物活性 | Acyclovir prevents bacterial infections during induction therapy for acute leukaemia. Acyclovir (Aciclovir) is a guanosine analogue and an orally active antiviral agent. Acyclovir inhibits HSV-1 (IC50 of 0.85 μM), HSV-2 (IC50 of 0.86 μM) and varicella-zoster virus. Acyclovir can be phosphorylated by viral thymidine kinase (TK), and Acyclovir triphosphate interferes with viral DNA polymerization through competitive inhibition with guanosine triphosphate and obligatory chain termination[1-4]. |
| In Vitro | Acyclovir (3-100 μM; 24-72 hours; Jurkat, U937, and K562 leukemia cells) treatment shows a dose- and time-dependent reduction of cell viability.Acyclovir (10-100 μM; 24-72 hours; Jurkat cells) treatment shows a delay/block in S phase and an increase of the sub-G1 peak.Acyclovir (10-100 μM; 24-72 hours; Jurkat cells) treatment activates caspase-3 and presences nuclear DNA fragmentation, thereby indicating apoptotic cell death[3].In HSV-infected cells, HSV thymidine kinase (HSV-TK) specifically phosphorylate Acyclovir to its monophosphate, and this activation confers a high degree of selectivity of the drugs. Thereafter, the monophosphate is further phosphorylated to the diphosphate (Acyclovir -DP) and triphosphate (Acyclovir -TP) by cellular kinases. The triphosphate is the fully activated metabolite that is toxic to the virus[4]. |
| In Vivo | Acyclovir (20 mg/kg; oral administration; three times daily; for 10 days; BALB/c mice) treatment in infected mice suppresses the development of skin lesions and results in a dissociation between DTH response and antibody production[1]. |
| 数据来源文献 |
[1]. Li Z, et al. Acyclovir treatment of skin lesions results in immune deviation in mice infected cutaneously with herpes simplex virus. Antivir Chem Chemother. 1999 Sep;10(5):251-7. [2]. Suzuki M, et al. Synergistic antiviral activity of acyclovir and vidarabine against herpes simplex virus types 1 and 2 and varicella-zoster virus. Antiviral Res. 2006 Nov;72(2):157-61. [3]. Benedetti S, et al. Acyclovir induces cell cycle perturbation and apoptosis in Jurkat leukemia cells, and enhances chemotherapeutic drug cytotoxicity. Life Sci. 2018 Dec 15;215:80-85. [4]. Hayashi K, et al. The role of a HSV thymidine kinase stimulating substance, scopadulciol, in improving the efficacy of cancer gene therapy. J Gene Med. 2006 Aug;8(8):1056-67. |
| 规格 | 20mg 10mM*1mL in DMSO 50mg |
| 单位 | 瓶 |
