产品名称: |
马立巴韦 |
中文别名: |
(2S,3s,4r,5s)-2-(5,6-二氯-2-(异丙基氨基)-1H-苯并[d]咪唑-1-基)-5-(羟基甲基)四氢呋喃-3,4-二醇;BENZIMIDAVIR 苯并咪唑核苷;马立巴韦;苯并咪唑核苷 |
英文名称: |
Maribavir |
英文别名: |
(2S,3S,4R,5S)-2-(5,6-Dichloro-2-(isopropylamino)-1H-benzo[d]imidazol-1-yl)-5-(hydroxymethyl)tetrahydrofuran-3,4-diol;(2S,3S,4R,5S)-2-(5,6-Dichloro-2-(isopropylamino)-1H-benzo[d]-imidazol-1-yl)-5-(hydroxymethyl)tetrahydrofuran-3,4-diol;(2S,3S,4R,5S)-2-[5,6-dichloro-2-(propan-2-ylamino)benzimidazol-1-yl]-5-(hydroxymethyl)oxolane-3,4-diol;1H-Benzimidazol-2-amine, 5,6-dichloro-N-(1-methylethyl)-1-β-L-ribofuranosyl-;1H-Benzimidazol-2-amine,5,6-dichloro-N-(1-methylethyl)-1-b-L-ribofuranosyl-;BENZIMIDAVIR;1263W94;BW1263W94;Bzurea;Camvia;Camvia (TN);Camvia(TM);GW257406X;Maribavir;5,6-Dichloro-N-(1-methylethyl)-1-beta-L-ribofuranosyl-1H-benzimidazol-2-amine;5,6-DICHLORO-2-ISOPROPYLAMINO-1-(-L-RIBOFURANOSYL)-LH-BENZIMIDAZOLE;5,6-DICHLORO-2-(ISOPROPYLAMINO)-1-(BETA-L-RIBOFURANOSYL)-1H-BENZIMIDAZOLE;BENZIMIDAVIR, 5,6-DICHLORO-2-(ISOPROPYLAMINO)-1-(β-L-RIBOFURANOSYL)-LH-BENZIMIDAZOLE;BENZIMIDAVIR: 5,6-DICHLORO-2-(ISOPROPYLAMINO)-1-(SS-L-RIBOFURANOSYL)-LH-BENZIMIDAZOLE;BW 1263W94;GW 257406X |
品牌: |
PERFEMIKER |
CAS号: |
176161-24-3 |
分子式: |
C15H19N3O4CL2 |
分子量: |
376.24 |
纯度: |
≥98% |
详细描述: |
<table class="table-cpd-info dsp" style="width: 1200px; border-collapse: collapse; border: 1px solid #bbbbbb; color: #333333; font-family: Helvetica, Arial, Verdana, 'Microsoft Yahei', STXihei, sans-serif; font-size: 16px; text-indent: 0px;"> <tbody> <tr> <td style="padding: 16px 16px 16px 15px; border-bottom: 1px dotted #bbbbbb; font-size: 14px; color: #333333; text-align: justify; line-height: 20px; width: 160px; font-weight: bold; border-right: 1px dotted #bbbbbb;"><span style="font-size: x-small;">产品描述</span></td> <td style="padding: 16px; border-bottom: 1px dotted #bbbbbb; color: #333333; text-align: justify; line-height: 20px;"><span style="font-size: x-small;">Maribavir is an orally available benzimidazole riboside compound with activity against cytomegalovirus (CMV). Maribavir is a selective ATP competitor of the viral UL97 kinase, which is involved in viral nuclear maturation events, such as viral DNA assembly and movement of viral capsids from the nucleus of infected cells. Maribavir has activity against strains of CMV that are resistant to standard anti-CMV agents.</span></td> </tr> <tr> <td style="padding: 16px 16px 16px 15px; border-bottom: 1px dotted #bbbbbb; font-size: 14px; color: #333333; text-align: justify; line-height: 20px; width: 160px; font-weight: bold; border-right: 1px dotted #bbbbbb;"><span style="font-size: x-small;">靶点活性</span></td> <td style="padding: 16px; border-bottom: 1px dotted #bbbbbb; color: #333333; text-align: justify; line-height: 20px;"><span style="font-size: x-small;">HCMV</span></td> </tr> <tr> <td style="padding: 16px 16px 16px 15px; border-bottom: 1px dotted #bbbbbb; font-size: 14px; color: #333333; text-align: justify; line-height: 20px; width: 160px; font-weight: bold; border-right: 1px dotted #bbbbbb;"><span style="font-size: x-small;">体外活性</span></td> <td style="padding: 16px; border-bottom: 1px dotted #bbbbbb; color: #333333; text-align: justify; line-height: 20px;"><span style="font-size: x-small;">Maribavir is a potent inhibitor of the autophosporylation of the wild type and all the major Ganciclovir (GCV) resistant UL97 mutants analysed with a mean IC50 of 35 nM. The M460I mutation results in hypersensitivity to Maribavir with an IC50 of 4.8 nM. A Maribavir resistant mutant of UL97 (L397R) is functionally compromised as both a Ganciclovir kinase and a protein kinase (~ 10% of wild type levels). Enzyme kinetic experiments demonstrate that Maribavir is a competitive inhibitor of ATP with a Ki of 10 nM[1]. Maribavir (1263W94) inhibits viral replication in a dose-dependent manner, with IC50 of 0.12±0.01 μM as measured by a multicycle DNA hybridization assay. The pUL97 protein kinase is strongly inhibited by Maribavir, with 50% inhibition occurring at 3 nM[2].</span></td> </tr> <tr> <td style="padding: 16px 16px 16px 15px; border-bottom: 1px dotted #bbbbbb; font-size: 14px; color: #333333; text-align: justify; line-height: 20px; width: 160px; font-weight: bold; border-right: 1px dotted #bbbbbb;"><span style="font-size: x-small;">激酶实验</span></td> <td style="padding: 16px; border-bottom: 1px dotted #bbbbbb; color: #333333; text-align: justify; line-height: 20px;"><span style="font-size: x-small;">Enzyme kinetic analysis is performed on the purified wild type and mutant UL97 protein species using increasing concentrations of ATP (2 μM to 20 μM). The amount of incorporated radiolabelled phosphate is plotted against the concentration of ATP in a Lineweaver Burke plot to determine the Km for ATP for each UL97 species. The effect of Maribavir upon the rate of radiolabelled phosphate incorporation by wild type or mutant UL97 is determined by protein kinase assays at a fixed concentration of Maribavir (0.5 μM) as above, or with increasing concentrations of Maribavir (0.01 μM to 5.0 μM) to determine the IC50 of Maribavir for each UL97 species. In order to determine the nature of the inhibition mediated by Maribavir, plots of 1/v vs 1/ATP with increasing concentrations of Maribavir are constructed. Competitive inhibition is evident if the family of lines cconverged on the y-axis at 1/Vmax. The change in slope caused by the addition of Maribavir is used to calculate the Ki[1].</span></td> </tr> <tr> <td style="padding: 16px 16px 16px 15px; border-bottom: 1px dotted #bbbbbb; font-size: 14px; color: #333333; text-align: justify; line-height: 20px; width: 160px; font-weight: bold; border-right: 1px dotted #bbbbbb;"><span style="font-size: x-small;">细胞实验</span></td> <td style="padding: 16px; border-bottom: 1px dotted #bbbbbb; color: #333333; text-align: justify; line-height: 20px;"><span style="font-size: x-small;">Maribavir (1263W94) is dissolved in DMSO and stored, and then diluted with appropriate media before use[2]. For these studies MRC-5 cells are seeded in 24-well plates at ~5×104 cells/well and grown for 3 days in MEM 8-1-1 to confluence (~1.1×105 cells/well). The cells are infected with AD169 in MEM 2-1-1 at an MOI ranging from 1 to 3 and incubated at 37°C for 90 min to allow viral adsorption. The unadsorbed virus is removed and replaced with 1 mL of MEM 2-1-1. To test the effect of compounds on viral DNA synthesis or maturation, Maribavir, BDCRB, or GCV is added to the medium at the concentrations indicated for each experiment[2].</span></td> </tr> </tbody> </table> <span style="font-size: x-small;">博飞美科的Maribavir,≥98%为酶抑制剂,产品稳定,定制速度快,极大地方便了广大科研客户的使用需求。产品包装为10mg。查询关键词:酶抑制剂,176161-24-3,Maribavir,≥98%,Maribavir,博飞美科,Perfemiker,上海,厂家直销。</span> |