Nevirapine (NSC 641530)

Catalog No.S1742

For research use only.

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

Nevirapine (NSC 641530) Chemical Structure

CAS No. 129618-40-2

Selleck's Nevirapine (NSC 641530) has been cited by 8 Publications

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Biological Activity

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

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
CEM-SS cells MnHhSpVv[3Srb36gZZN{[Xl? NHn2W|RCdnSrdnnyZYwh[WO2aY\peJkh[WejaX7zeEBJUVZzIGLGJIlvKEOHTT3TV{Bk\WyuczDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oII\pdpV{NWmwZIXj[YQh[3m2b4DheIhq[yCnZn\lZ5Qh[nliWGTUJIF{e2G7LDDFR|UxRTFwNTDuUS=> NETqW3IyQDJ{MkC4PC=>
human MT4 cells Mny0SpVv[3Srb36gZZN{[Xl? NXjSTYY3SW62aY\pdoFtKGGldHn2bZR6KGGpYXnud5QhUHWvYX6gbY1ufW6xZHXmbYNq\W6leTD2bZJ2eyBzIIP1ZpR6eGViQzDpcoZm[3SnZDDpckBpfW2jbjDNWFQh[2WubIOgZZN{\XO|ZXSgZZMhemWmdXP0bY9vKGmwII\pdpV{KGmwZIXj[YQh[3m2b4DheIhq[2m2eTygSWM2OD1yLkCwOFg5KM7:TR?= MYWxPVk{Ozd7Nx?=
human Jurkat E6-1 cells NGC0XpNHfW6ldHnvckBie3OjeR?= NVrIV5Z7OiCmYYnz NIjTSFRCdnSrdnnyZYwh[WO2aY\peJkh[WejaX7zeEBJUVZzIFXuek1xe2W3ZH;2bZJ2eyCrbn\lZ5Rm\CCrbjDoeY1idiCMdYLrZZQhTTZvMTDj[YxteyCjZoTldkAzKGSjeYOgZpkhdHWlaX\ldoF{\SCjc4PhfUwhUUN3ME2wMlA1KM7:TR?= NGTzV4IzOTRzNEe3Oi=>
human C1866 cells NF\EcZdEgXSxdH;4bYNqfHliYYPzZZk> M3TaeVczKGh? MV;DfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDDNVg3PiClZXzsd{Bi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBGSzVyPUCuNFQ6PDNizszN MnrNNlEyQTR7M{m=
human MT2 cells MnfWSpVv[3Srb36gZZN{[Xl? MmDrOEBl[Xm| MkPDRY51cX[rcnHsJIFkfGm4aYT5JIFo[Wmwc4Sge4lt\CC2eYDlJGhKXjFiM1KgbY5n\WO2ZXSgbY4hcHWvYX6gUXQzKGOnbHzzJIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[gdFI1KGGwdHnn[Y4heHKxZIXjeIlwdiCjZoTldkA1KGSjeYOgZpkhTUyLU1GsJGVEPTB;MD6wOVMh|ryP M3TDT|IxPTJ5OUey
HeLa cells NYfyZXE5TnWwY4Tpc44h[XO|YYm= Ml7kRY51cX[rcnHsJIFkfGm4aYT5JIFo[Wmwc4Sge4lt\CC2eYDlJGhKXjFiaX6gTIVN[SClZXzsd{BjgSCPQVfJJIF{e2G7LDDJR|UxRTBwMEWzJO69VQ>? M{HKOFE5PjZ3NUiz
293T cells NEfSWJdHfW6ldHnvckBie3OjeR?= MVLJcohq[mm2aX;uJI9nKHerbHSgeJlx\SCKSW[xJJJmfmW{c3WgeJJidnOlcnnweIF{\SCrbjCyPVNVKGOnbHzzMEBKSzVyPUCuNFYh|ryP M121fVE3PTJ5NEi0
MDCK2 cells MXjGeY5kfGmxbjDhd5NigQ>? NGDB[YgyOCEQvF2= M2jJT2lvcGmkaYTpc44hd2ZiaIXtZY4hVVKSMjDlfJBz\XO|ZXSgbY4hVUSFS{KgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5kemWjc3WgbY4hcW62cnHj[YxtfWyjcjDDUWYh\my3b4Lld4NmdmOnIHH0JFExKHWPIHL5JGNOTkSDIHHzd4F6 MXSxO|E4OjNzMR?=
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]

Protocol (from reference)

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 266.3
Formula

C15H14N4O

CAS No. 129618-40-2
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=C2C(=NC=C1)N(C3=C(C=CC=N3)C(=O)N2)C4CC4

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

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
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02738502 Completed Drug: darunavir monotherapy Maternal-fetal Infection Transmission ANRS Emerging Infectious Diseases|Institut National de la Santé Et de la Recherche Médicale France July 6 2016 Phase 2
NCT02447159 Completed Behavioral: Conditional Cash Transfers HIV|HIV Infections|Pregnancy|Infant Newborn Diseases University of California San Francisco|University of California Berkeley|New Incentives|Bill and Melinda Gates Foundation August 2015 Not Applicable
NCT02429791 Active not recruiting Drug: DTG 50 mg|Drug: RPV 25 mg|Drug: CAR HIV Infections ViiV Healthcare|Janssen Pharmaceuticals|GlaxoSmithKline April 14 2015 Phase 3
NCT02422797 Active not recruiting Drug: DTG 50 mg|Drug: RPV 25 mg|Drug: CAR HIV Infections ViiV Healthcare|Janssen Pharmaceuticals|GlaxoSmithKline April 21 2015 Phase 3
NCT03023033 Completed Behavioral: mHealth messaging|Behavioral: Transport Payments HIV|AIDS Elizabeth Glaser Pediatric AIDS Foundation|Population Council|Ministry of Health Tanzania October 2014 Not Applicable

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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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