Name: Nevirapine (NSC 641530)
Brand: Selleck Chemicals
SKU: S1742
Rating: 5 (15 reviews)

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Kwaliteitscontrole (Quality Control)

Batch: Zuiverheid: 99.66%

99.66

Gerelateerde doelwitten	Integrase Bacterial Antibiotics Anti-infection Fungal Antiviral COVID-19 Parasite HIV HCV Protease
Overig Reverse Transcriptase Inhibitoren	Dapivirine (TMC120) Fangchinoline Salicylanilide 3'-Fluoro-3'-deoxythymidine (Alovudine) Ulonivirine Lersivirine (UK-453061) Bifendate 4-Chloro-2-(trifluoroacetyl)aniline hydrochloride Islatravir

Celkweek, behandeling & werkzame concentratie
(Cell Culture, Treatment & Working Concentration)

Cellijnen	Assaytype	Concentratie	Incubatietijd	Activiteitsbeschrijving
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
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
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
human C1866 cells	Cytotoxicity assay		72 h	Cytotoxicity against human C1866 cells after 72 hrs by MTT assay, EC50=0.04943 μM
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
HeLa cells	Function assay			Antiviral activity against wild type HIV1 in HeLa cells by MAGI assay, IC50=0.053 μM
293T cells	Function assay			Inhibition of wild type HIV1 reverse transcriptase in 293T cells, IC50=0.06 μM
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
Klik om meer experimentele gegevens over cellijnen te bekijken

Chemische informatie, opslag en stabiliteit (Chemical Information, Storage & Stability)

Molecuulgewicht	266.3	Formule	C₁₅H₁₄N₄O	Opslag (vanaf de datum van ontvangst)	3 jaar-20°Cpoeder
CAS-nr.	129618-40-2	SDF downloaden		Opslag van stamoplossingen	1 jaar-80°Cin oplosmiddel 1 maand-20°Cin oplosmiddel
Synoniemen	NSC 641530,NVP			Smiles	CC1=C2C(=NC=C1)N(C3=C(C=CC=N3)C(=O)N2)C4CC4

Oplosbaarheid (Solubility)

In vitro
Batch:

DMSO : 53 mg/mL (199.02 mM)
(Met vocht verontreinigd DMSO kan de oplosbaarheid verminderen. Gebruik verse, watervrije DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molariteitscalculator

Massa	Concentratie	Volume	Molecuulgewicht
=	×	×

Verdunningscalculator Molecuulgewichtcalculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Gevalideerd door Selleck labs. Mocht u aanpassingen aan deze formulering nodig hebben, neem dan contact op met ons verkoopteam voor aangepaste tests.	2.600mg/ml (9.76mM)	Taking the 1 mL working solution as an example, add 50 μL of 52 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Gevalideerd door Selleck labs. Mocht u aanpassingen aan deze formulering nodig hebben, neem dan contact op met ons verkoopteam voor aangepaste tests.	0.660mg/ml (2.48mM)	Taking the 1 mL working solution as an example, add 50 μL of 13.2 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo formulatiecalculator (heldere oplossing)

Stap 1: Voer onderstaande informatie in (Aanbevolen: een extra dier om rekening te houden met verlies tijdens het experiment)

Dosering: mg/kg Gemiddeld gewicht van dieren: g Doseervolume per dier:μL Aantal dieren:

Stap 2: Voer de in vivo formulering in (Dit is alleen de calculator, geen formulering. Neem eerst contact met ons op als er geen in vivo formulering is in de sectie oplosbaarheid.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Berekeningsresultaten:

Werkconcentratie: mg/ml;

Methode voor het bereiden van DMSO-moedervloeistof: mg geneesmiddel vooropgelost in μL DMSO ( Concentratie moedervloeistof mg/mL, Neem eerst contact met ons op als de concentratie de DMSO-oplosbaarheid van de batch van het geneesmiddel overschrijdt. )

Methode voor het bereiden van in vivo formulering: Neem μL DMSO moedervloeistof, voeg daarna toeμL PEG300, mengen en verhelderen, daarna toevoegenμL Tween 80, mengen en verhelderen, daarna toevoegen μL ddH₂O, mengen en verhelderen.

Methode voor het bereiden van in vivo formulering: Neem μL DMSO moedervloeistof, voeg daarna toe μL Maïsolie, mengen en verhelderen.

Opmerking: 1. Zorg ervoor dat de vloeistof helder is voordat u het volgende oplosmiddel toevoegt.
2. Zorg ervoor dat u het/de oplosmiddel(en) in de juiste volgorde toevoegt. U moet ervoor zorgen dat de verkregen oplossing, bij de vorige toevoeging, een heldere oplossing is voordat u verdergaat met het toevoegen van het volgende oplosmiddel. Fysieke methoden zoals vortexen, ultrasoon of een warmwaterbad kunnen worden gebruikt om het oplossen te bevorderen.

Werkingsmechanisme (Mechanism of Action)

Targets/IC₅₀/Ki	Reverse transcriptase
In vitro	Nevirapine (NSC 641530) is a non-nucleoside RT inhibitor with a well-characterized inhibitory activity on RT enzymes of retroviral origin. It is also an effective inhibitor of the endogenous RT in murine and human cell lines. This compound 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. It alters the cleavage specificity of the RNase H, resulting in Nevirapine-induced stimulation of RNase H activity beyond the increase expected from the change in cleavage specificity. It is an inhibitor of only CYP3A4 at concentrations that are well above those of therapeutic relevance (Ki = 270 mM). Its 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.
In vivo	Nevirapine (NSC 641530) is metabolized to 4-CANVP as a major metabolite in all male animals and in female mice, dogs, and monkeys. 3-OHNVP is a major fecal metabolite in all animals except for the male rat. In the bile of rats, 4-CANVP is a major metabolite along with 12-OHNVP glucuronide.
Referenties	[1] https://pubmed.ncbi.nlm.nih.gov/10570031/ [2] https://pubmed.ncbi.nlm.nih.gov/12747369/ [3] https://pubmed.ncbi.nlm.nih.gov/1371691/ [4] https://pubmed.ncbi.nlm.nih.gov/7533167/ [5] https://pubmed.ncbi.nlm.nih.gov/10570025/

Informatie over klinische proeven (Clinical Trial Information)

(gegevens van https://clinicaltrials.gov, bijgewerkt op 2024-05-22)

NCT-nummer	Werving	Aandoeningen	Sponsor/medewerkers	Startdatum	Fasen
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	--

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Nevirapine (NSC 641530) Reverse Transcriptase Remmer

Molecuulgewicht: 266.3

Kwaliteitscontrole (Quality Control)

Celkweek, behandeling & werkzame concentratie
(Cell Culture, Treatment & Working Concentration)

Chemische informatie, opslag en stabiliteit (Chemical Information, Storage & Stability)

Oplosbaarheid (Solubility)

Molariteitscalculator

In vivo formulatiecalculator (heldere oplossing)

Werkingsmechanisme (Mechanism of Action)

Informatie over klinische proeven (Clinical Trial Information)

Nevirapine (NSC 641530) Reverse Transcriptase Remmer

Molecuulgewicht: 266.3

Kwaliteitscontrole (Quality Control)

Celkweek, behandeling & werkzame concentratie (Cell Culture, Treatment & Working Concentration)

Chemische informatie, opslag en stabiliteit (Chemical Information, Storage & Stability)

Oplosbaarheid (Solubility)

Molariteitscalculator

In vivo formulatiecalculator (heldere oplossing)

Werkingsmechanisme (Mechanism of Action)

Informatie over klinische proeven (Clinical Trial Information)

Celkweek, behandeling & werkzame concentratie
(Cell Culture, Treatment & Working Concentration)