计算溶液所需的质量、体积或浓度。
为什么选择此级别
，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
Dapivirine (TMC120)是一种非核苷类抑制剂，作用于HIV逆转录酶，IC50为24 nM，抑制多种不同类型的HIV-1分离株，包括多种耐NNRTI的分离株。
Information
Dapivirine (TMC120) Dapivirine (TMC120) is a non-nucleoside inhibitor for HIV reverse transcriptase with IC50 of 24 nM, inhibits a broad panel of HIV-1 isolates from different classes, inclucing a wide range of NNRTI-resistant isolates. Phase 3.
In vitro
Dapivirine prevents HIV-induced syncytium formation in the nanomolar range and shows a low cytostatic activity. Dapivirine apparently blocks HIV-1 infection in the primary cultures at a 10 nM concentration, but secondary cultures reveals that a 100 nM concentration is needed to completely prevent proviral integration. Dapivirine is well tolerated by epithelial cells, T cells, macrophages, and cervical tissue explants with CC50 (50% cytotoxic concentration) of 10 μM to 20 μM. Dapivirine potently inhibits infection by both X4- and R5-utilizing HIV-1 strains with IC50 of 1.46 nM in cell-based assays. Dapivirine potently inhibits HIV-1BaL infection of human ectocervical explant tissue in a dose-dependent manner, as evaluated by the reduction in both p24 release and provirus content in cultured explants. Dapivirine inhibits the transmission of virus to permissive T cells in a dose-dependent manner, with an IC50 of 0.1 nM. Dapivirine results in significant inhibition of HIV infection when explants are challenged with virus immediately with IC90 of 100 nM. Dapivirine is also able to inhibit viral dissemination by migratory cells.
In vivo
Dapivirine-containing gel at vaginal level inhibits cell-associated HIV infection in mice. More placebo (7 of 12) than Dapivirine (3 of 24) gel users has positive vaginal swab results, with white blood cells being the most common finding. Dapivirine (0.05%) results in Cmax of 715 pg/mL, AUC of 15 ng×h/mL and T1/2 of 89.87 hours in plasma after 14 days post-dose. Mean Dapivirine (0.05%) concentrations in vaginal fluids collected at the introitus, mid vagina, and cervix are in the range of 62-265 μg/g on day 1.
Cell Data
cell lines：Human renal proximal tubule epithelial (RPTE) cells
Concentrations：
Incubation Time：
Powder Purity:≥100%
规格
别名
达匹韦林 (TMC120)
英文别名
Benzonitrile, 4-[[4-[(2,4,6-trimethylphenyl)amino]-2-pyrimidinyl]amino]-
规格或纯度
10mM in DMSO
英文名称
Dapivirine (TMC120)
生化机理
达匹韦林（TMC120）是一种非核苷类艾滋病毒逆转录酶抑制剂，其 IC50 值为 24 nM，可抑制多种不同类别的 HIV-1 分离物，包括多种耐 NNRTI 的分离物。第 3 阶段。
储存条件
-80℃储存
运输条件
特低温运输
作用类型
抑制剂
作用机制
逆转录酶抑制剂
名称和识别符
EC号
688-158-2
分子类型
小分子
Isomeric SMILES
CC1=CC(=C(C(=C1)C)NC2=NC(=NC=C2)NC3=CC=C(C=C3)C#N)C
分子量
329.4
Reaxy-Rn
8934631
Reaxys-RN link address
https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=8934631&ln=
技术文档
高级数据
产品属性
| ALogP | 4.8 |
|---|
安全和危险性（GHS）
象形图
信号词
Warning
危险声明
H302: 吞食有害
预防措施声明
P501: 将内容物/容器处理到。。。
P264: 处理后要彻底洗手。
P270: 使用本产品时，请勿进食、饮水或吸烟。
P330: 漱口
P301+P317: 如果被吞咽：请寻求医疗帮助。
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
溶液计算器
产品仅提供给经过验证的企业、机构和合格的专业人员用于研发。不适用于人类、动物、诊断或治疗。
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