| CAS |
113852-37-2 |
| Chinese Name |
西多福韦 |
| English Name |
Cidofovir |
| Synonyms |
(S)-[[2-(4-氨基-2-氧-1(2H)嘧啶基)-1-(羟基甲基)乙氧基]甲基]膦酸;培哚普利叔丁胺盐 |
| Molecular Formula |
C8H14N3O6P |
| Molecular Weight |
279.19 |
| Solubility |
Soluble in Water |
| Purity |
≥98% |
| Appearance |
White to off-white Solid |
| Storage |
Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| EC |
EINECS 638-807-0 |
| MDL |
MFCD00866936 |
| SMILES |
OC[C@@H](OCP(O)(O)=O)CN1C=CC(N)=NC1=O |
| InChIKey |
VWFCHDSQECPREK-LURJTMIESA-N |
| InChI |
InChI=1S/C8H14N3O6P/c9-7-1-2-11(8(13)10-7)3-6(4-12)17-5-18(14,15)16/h1-2,6,12H,3-5H2,(H2,9,10,13)(H2,14,15,16)/t6-/m0/s1 |
| PubChem CID |
60613 |
| Target Point |
DNA/RNA Synthesis inhibitor |
| Passage |
Cell Cycle;DNA Damage/DNA Repair |
| Background |
Cidofovir can control cytomegalovirus CMV replication by inhibiting viral DNA polymerase activity. |
| In Vitro |
Cidofovir处理培养的细胞，抑制人类巨细胞病毒(HCMV)感染。Cidofovir抑制巨细胞病毒(CMV)蚀斑形成，即使是感染后48小时后加入到细胞中，作用于Davis和AD-169株时IC50分别为0.9 μg/mL和1.6 μg/mL。[1] Cidofovir也抑制单纯疱疹病毒感染。此外，Cidofovir作用于猴肾细胞，抑制HSV-1诱导的细胞融合，也抑制HSV-1特异性蛋白的表达和病毒DNA的合成。[3] |
| In Vivo |
Cidofovir 每天按5 mg/kg剂量皮下注射给药受感染的豚鼠，持续给药5天，显著降低血，脾，肺，和唾液腺中病毒传染力。Cidofovir处理受感染的动物，显著降低淋巴细胞增多和脾脏的平均组织指数。[2] Cidofovir作用于皮内感染与HSV-1或HSV-2的无毛小鼠，抑制所有临床表现(皮肤损伤，后腿瘫痪，和死亡)。Cidofovir最显著的特点是感染后到直至第4天才单独给药，也显著抗HSV-1或HSV-2感染。[4] Cidofovir作用于皮下移植小鼠黑色素瘤B16细胞的C57B16/J小鼠，抑制产生的高度侵袭性的黑色素瘤的生长。[5] |
| Animal Experiment |
Mice were treated daily with systemic cidofovir at several doses. In treated and control groups，tumour growth was measured using a calliper，and histological studies were performed.In untreated mice，massive invasive melanoma tumours were observed on day 5 after tumour cell grafting. Cidofovir treatment gave a dose-dependent reduction in tumour size. Tumour growth was inhibited by 62% at a dose of 37.5 mg kg(-1)three times weekly，as compared with control mice treated with saline alone. At 67 mg kg(-1)three times weekly，tumour growth was inhibited by 90%. Increasing the cidofovir dose to 50 or 100 mg kg(-1)daily resulted in a gradual increase in the antitumoral effect of the compound. In one experiment，cidofovir was administered at 100 mg kg(-1)five times weekly from the eighth day after the injection of tumour cells，when the tumour already had a volume of approximately 100 mm(3). In the treatment group，on the 14th day the tumour volume was approximately 200 mm(3)，while in the control group it had increased to 750 mm(3).[5] |
| Data Literature Source |
[1] Snoeck R，et al，Antimicrob Agents Chemother，1988，32(12)，1839-1844.
[2] Li SB，et al. Antiviral Res，1990，13(5)，237-252.
[3] Chatterjee S，et al. Antiviral Res.，1992，19(3)，181-192.
[4] De Clercq E，et al. Antimicrob Agents Chemother，1991，35(4)，701-706.
[5] Redondo P，et al. Br J Dermatol，2000，143(4)，741-748. |
| Unit |
Piece |
| Specification |
10mg 50mg |
English
中文
Manual Download
