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Nevirapine (NSC 641530)

Name: Nevirapine (NSC 641530)
Brand: Selleck Chemicals
SKU: S1742
Rating: 5 (10 reviews)

Synonyms: NSC 641530,NVP

Catalog No.S1742 Purity: 100%

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

CAS: 129618-40-2

Selleck's Nevirapine (NSC 641530) has been cited by 10 Publications

1 Customer Review

Purity & Quality Control

Batch: Purity: 100%

100

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Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	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
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-01-11)
NCT05725252	Not yet recruiting	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	--

References

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Chemical lnformation & 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)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

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
Batch:

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In vivo Formulation Calculator

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In vivo Formulation Calculator (Clear solution)

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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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
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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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