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Nevirapine

SKU: orb1308075

Description

Nevirapine is a non-nucleoside reverse transcriptase inhibitor used in HIV research. It is applied in vitro and in vivo to study viral replication inhibition, combination antiretroviral therapy efficacy, and mechanisms of drug resistance.

Research Area

Infectious Disease & Virology, Protein Biochemistry

Images & Validation

Key Properties

CAS Number129618-40-2
MW266.3
Purity99.59%
FormulaC15H14N4O
SMILESCC1=CC=NC2=C1NC(=O)C1=C(N=CC=C1)N2C1CC1
TargetReverse Transcriptase,Parasite,HIV Protease
SolubilityDMSO:22.73 mg/mL (85.35 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (3.76 mM);Ethanol:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

Target IC50
HIV-1:270 μM(ki)
In Vivo
Nevirapine (NVP) acts primarily as a CYP3A4 inhibitor, with its inhibitory concentration significantly higher than the concentration related to its therapeutic use (Ki: 270 μM). As a non-nucleoside reverse transcriptase inhibitor, Nevirapine effectively inhibits reverse transcriptase from retroviruses, and it also inhibits endogenous reverse transcription in both mouse and human cell lines. Additionally, Nevirapine has been shown to alleviate the differentiation block in cell lines and primary cells from acute myeloid leukemia (AML) patients, as indicated by morphological, functional, and immunophenotypic analyses. It alters the cleavage specificity of RNAse H, resulting in Nevirapine-induced RNase H activity that exceeds the expected changes in cleavage specificity. Nevirapine is a highly specific inhibitor of HIV-1 reverse transcriptase (RT), with an IC50 of 84 nM in enzyme assays and an IC50 of 40 nM against HIV-1 replication in cell cultures.
In Vitro
In various animal models, the metabolism of Nevirapine (NVP) proceeds as follows: One of the primary metabolites identified in the feces of all tested animals, except male rats, is 3-HydroxylNVP (3-OHNVP). For all male subjects as well as female mice, dogs, and monkeys, one of the principal metabolites is 4-Carboxylic AcidNVP (4-CANVP). Additionally, the predominant metabolites in rat bile are found to be 4-CANVP and a glucuronide conjugate of 12-HydroxylNVP (12-OHNVPglucuronide).
Cell Research
FRO cells are seeded into 96-well culture plates at 10,000 cells/well. Cells are treated with different doses of nevirapine (0, 100, 200, 350 and 500 μM) for 48 h. MTT dye (5 mg/mL) is added to each well for additional 4 h, and the reaction is then stopped by the addition of DMSO. Optical density is measured at 490 nm on a multi-well plate reader.

Storage & Handling

StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

BI-RG 587, BI-RG587, BI-RG-587, Inhibitor, HIV, HIV Protease, HIV-1 reverse transcriptase, HIVProtease, Human immunodeficiency virus, NSC 641530, inhibit, NSC641530, NSC-641530, Nevirapine, NVP, Reverse Transcriptase, ReverseTranscriptase

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Key Properties

No computed properties available.

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Nevirapine (orb1308075)

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% DMSO +
%+
% Tween 80 +
%

Available Sizes

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5 mg
$ 80.00
1 ml x 10 mM (in DMSO)
$ 90.00
10 mg
$ 90.00
50 mg
$ 100.00
100 mg
$ 130.00
200 mg
$ 130.00
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