Home Microbiology Reverse Transcriptase inhibitor Nevirapine (NSC 641530) For research use only.

Nevirapine (NSC 641530)

Synonyms: NSC 641530,NVP

Nevirapine (NSC 641530,NVP) is a non-nucleoside reverse transcriptase inhibitor (NNRTI) used to treat HIV-1 infection and AIDS.

Nevirapine (NSC 641530) Chemical Structure

Nevirapine (NSC 641530) Chemical Structure

CAS No. 129618-40-2

Purity & Quality Control

Nevirapine (NSC 641530) Related Products

Signaling Pathway

Reverse Transcriptase Signaling Pathways

Reverse Transcriptase Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
CEM-SS cells Function assay Antiviral activity against HIV1 RF in CEM-SS cells assessed as inhibition of virus-induced cytopathic effect by XTT assay, EC50=1.5 nM 18222088
human MT4 cells Function assay Antiviral activity against Human immunodeficiency virus 1 subtype C infected in human MT4 cells assessed as reduction in virus induced cytopathicity, EC50=0.00488 μM 19933797
human Jurkat E6-1 cells Function assay 2 days Antiviral activity against HIV1 Env-pseudovirus infected in human Jurkat E6-1 cells after 2 days by luciferase assay, IC50=0.04 μM 21414776
human C1866 cells Cytotoxicity assay 72 h Cytotoxicity against human C1866 cells after 72 hrs by MTT assay, EC50=0.04943 μM 21194939
human MT2 cells Function assay 4 days Antiviral activity against wild type HIV1 3B infected in human MT2 cells assessed as inhibition of p24 antigen production after 4 days by ELISA, EC50=0.053 μM 20527972
HeLa cells Function assay Antiviral activity against wild type HIV1 in HeLa cells by MAGI assay, IC50=0.053 μM 18665583
293T cells Function assay Inhibition of wild type HIV1 reverse transcriptase in 293T cells, IC50=0.06 μM 16527484
MDCK2 cells Function assay 10 μM Inhibition of human MRP2 expressed in MDCK2 cells assessed as increase in intracellular CMF fluorescence at 10 uM by CMFDA assay 17172311
Click to View More Cell Line Experimental Data

Biological Activity

Description Nevirapine (NSC 641530,NVP) is a non-nucleoside reverse transcriptase inhibitor (NNRTI) used to treat HIV-1 infection and AIDS.
Targets
Reverse transcriptase [1]
In vitro
In vitro

Nevirapine (NVP) itself is an inhibitor of only CYP3A4 at concentrations that are well above those of therapeutic relevance (Ki = 270 mM). [1] 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. [2] 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. [3] 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. [4]
In Vivo
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. [5]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05725252 Completed
Healthy Volunteers
NVP Healthcare
 May 28 2023 Phase 1
NCT05354713 Completed
Healthy Volunteers
NVP Healthcare
 November 5 2022 Phase 1
NCT04926727 Unknown status
Nausea Gravidarum|Vomiting of Pregnancy
Italfarmaco|Opera CRO a TIGERMED Group Company
 October 4 2021 --
NCT02738502 Completed
Maternal-fetal Infection Transmission
ANRS Emerging Infectious Diseases|Institut National de la Santé Et de la Recherche Médicale France
 July 6 2016 Phase 2
NCT02383849 Completed
Low-Birth-Weight Infant|Tuberculosis|HIV
International Maternal Pediatric Adolescent AIDS Clinical Trials Group|National Institute of Allergy and Infectious Diseases (NIAID)|Eunice Kennedy Shriver National Institute of Child Health and Human Development (NICHD)
 August 4 2015 --

Chemical Information & Solubility

Molecular Weight 266.3 Formula

C15H14N4O
CAS No. 129618-40-2 SDF Download Nevirapine (NSC 641530) SDF
Smiles CC1=C2C(=NC=C1)N(C3=C(C=CC=N3)C(=O)N2)C4CC4
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 53 mg/mL ( (199.02 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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