中文名:奈韦拉平
英文名:Nevirapine (NSC 641530)
英文别名:11-cyclopropyl-5,11-dihydro-4-methyl-6H-dipyrido[3,2-b:2',3'-e][1,4]diazepin-6-one
纯度:10mM in DMSO
货号:N408013
包装:1ml
Cas号:129618-40-2
存储温度:-80℃储存
产品介绍:
Information
Nevirapine (NSC 641530) Nevirapine (NSC 641530) is a non-nucleoside reverse transcriptase inhibitor (NNRTI) used to treat HIV-1 infection and AIDS.
In vitro
Nevirapine (NVP) itself is an inhibitor of only CYP3A4 at concentrations that are well above those of therapeutic relevance (Ki = 270 mM). Nevirapine is a non-nucleoside RT inhibitor with a well-characterized inhibitory activity on RT enzymes of retroviral origin. Nevirapine is also an effective inhibitor of the endogenous RT in murine and human cell lines. Nevirapine exposure rescues the differentiation block present in acute myeloid leukemia (AML) cell lines and primary blasts from two AML patients, as indicated by morphological, functional and immunophenotypic assays. Nevirapine, a dipyridodiazepinone, is a highly specific inhibitor of HIV-1 reverse transcriptase (RT) which exhibits an IC50 = 84 nM in enzyme assays and IC50 = 40nM against HIV-1 replication in cell culture. Nevirapine alters the cleavage specificity of the RNase H, resulting Nevirapine-induced stimulation of RNase H activity beyond the increase expected from the change in cleavage specificity.
In vivo
4-CANVP is a major metabolite in all the male animals and the female mouse, dog, and monkey. 3-OHNVP is a major fecal metabolite in all animals except for the male rat. 4-CANVP is a major metabolite along with 12-OHNVP glucuronide in the bile of rats.
Cell Data
cell lines:Pancreatic cancer cell lines (HcG25, Panc89, PA-TU8988T, Panc2.13, MiaPaCa2, Panc10.05, Panc8.13, BxPC-3, etc.)
Concentrations:
Incubation Time:
Powder Purity:≥99%
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关键字: 11-?cyclopropyl-?5,?11-?dihydro-?4-?methyl-6H-?dipyrido[3,?2-?b:2',?3'-?e]?[1,?4]?diazepin-?6-?one
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