Ribavirin 利巴韦林(病毒唑)


描述

Ribavirin 利巴韦林(病毒唑)

产品关键词:

Ribavirin 利巴韦林;Virazole 病毒唑;Ribavirin 5′-phosphate 利巴韦林5’-磷酸;Antiviral agent 抗病毒剂;肌苷单磷酸(IMP)脱氢酶;CAS:36791-04-5;

产品信息                                                                                                            

产品名称 产品编号               规格                   价格(元)          
Ribavirin 利巴韦林(病毒唑)         MS0043-1G 1g 198
Ribavirin 利巴韦林(病毒唑) MS0043-5G 5g 498
Ribavirin 利巴韦林(病毒唑) MS0043-25G 25g 1488

【温馨提示】:见我司(MKBio)的小分子化合物常见问题-金畔生物

产品描述          产品描述

利巴韦林(Ribavirin),俗称病毒唑,一种具广谱抗病毒特性的鸟苷类似物,靶向包括呼吸道合胞病毒(RSV)、丙型肝炎病毒(HCV)和流感病毒在内的DNA和RNA病毒。利巴韦林是一种药物前体,能够被细胞内激酶单磷酸或三磷酸化而激活。这些磷酸化衍生物对细胞和病毒内的酶产生各种效应,引起病毒复制的抑制。利巴韦林结合并重新分布哺乳动物eIF4E从细胞核到细胞质(Ki~ 0.3 μM,利巴韦林三磷酸,活性代谢物)。能够抑制原代AML-M5祖细胞的克隆形成(IC50~1 μM),还能减缓急性髓细胞性白血病(AML)的疾病严重程度。

产品特性

1)   CAS NO:36791-04-5

2)   化学名:1-β-D-ribofuranosyl-1H-1,2,4-triazole-3-carboxamide 1-β-D-呋喃核糖-1,2,4-三氮唑-3-羟酰胺

3)   英文同义名:NSC-163039, ICN-1229, RTCA, Tribavirin, Ribasphere, Rebetol, Virazole, Copegus;

4)   中文同义名:病毒唑,三氮唑核苷,三唑核苷;

5)   分子式:C8H12N4O5

6)   分子量:244.21 g/mol

7)   外观:白色或类白色结晶性粉末

8)   纯度:>99%

9)   溶解性:溶于水(≥20mg/ml),DMSO(≥20mg/ml),不溶于乙醇、乙醚、二氯甲烷

10)化学结构式:

保存与运输方法

保存:室温干燥保存,可置于-20°C长期干燥保存,3年有效。

运输:室温运输。

注意事项

1)  关于化合物溶解说明:化合物溶解性比如≥20mg/ml,说明至少有20mg/ml的溶解度,但不确定最大饱和溶解度。化合物的溶解度会因生产厂家和批次不同产生差异,具体以实际测试为准。

2)  本品并非商业化药物,仅限科研用途,不可用于临床或诊疗用途。

3)   为了您的安全和健康,请穿实验服并戴一次性手套操作。

配制储存液

         质量

溶剂体积          

浓度

1mg 5mg 10mg 100mg
1mM 4.0949 mL            20.4743 mL        40.9486 mL         409.4836 mL      
5mM 0.8190 mL 4.0949 mL 8.1897 mL 81.8967 mL
10mM 0.4095 mL 2.0474 mL 4.0949 mL 40.9484 mL
50mM 0.0819 mL 0.4095 mL 0.8190 mL 8.1897 mL

使用方法【源自文献,仅作参考】

文献1,Chang J et al. Combination of alpha-glucosidase inhibitor and ribavirin for the treatment of Dengue virus infection in vitro and in vivo. Antiviral Res. 2011 Jan;89(1):26-34. PMID: 21073903

体内研究:

动物模型(Animal Model):DENV (serotype 2, TSV01 strain) infected mice

给药剂量(Dosages):The mice were challenged with DENV (serotype 2, TSV01 strain), at 5×106pfu/mouse via i.p. injection. Imino sugar (CM-10-18) was given orally at 75mg/kg twice daily at 12 hr intervals, andribavirin was given orally at 40mg/kg once daily, for 3 consecutive days post-infection. PBS was given to control mice.Blood samples were drawn 3 days post-infection for determination of plasma virus titer by plaque assay.

实验结果(Results):While ribavirin at 40mg/kg by itself did not reduce viremia, and 75 mg/kg of CM-10-18 treatment only modestly reduced the viremia by 1.9-fold, combination of the two compounds reduced the viremia by 4.7-fold.

文献2,Kentsis A et al. Ribavirin suppresses eIF4E-mediated oncogenic transformation by physical mimicry of the 7-methyl guanosine mRNA cap. Proc Natl Acad Sci U S A. 2004 Dec 28;101(52):18105-10. PMID: 15601771

体内研究:

动物模型(Animal Model):Female 5- to 7-week old athymic NCr-nu/nu mice

药物配制(Preparation):For treatments, drugs were dissolved in PBS (pH 7.4) and filter-sterilized. Untreated cells and animals received filter-sterilized PBS.

给药剂量(Dosages):Nude mice were engrafted by using sub-cutaneous injection of eIF4E-dependent FaDu cells andtreated with 40 μg/kg ribavirin orally each day, yielding a mean body concentration of ≈1 μM.Photograph of tumors resectedafter 20 days of treatment.

实验结果(Results):After 20 days of ribavirin treatment, mean tumor volume of animals in the treatment group was 6-fold less than those in the untreated control group. At this low concentration, ribavirin was apparently well tolerated and minimally toxic as suggested by the absence of treatment-associated mortality and of effect on body weight.