Nevirapine (NSC 641530)

Catalog No.S1742 Batch:S174202

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Technical Data

Formula

C15H14N4O
Molecular Weight 266.3 CAS No. 129618-40-2
Solubility (25°C)* In vitro DMSO 53 mg/mL (199.02 mM)
Water Insoluble
Ethanol Insoluble
In vivo (Add solvents to the product individually and in order)
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 40%PEG300 5%Tween80 50%ddH2O

Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.

 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 95% Corn oil

Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.

 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. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description Nevirapine (NSC 641530,NVP), a non-nucleoside reverse transcriptase inhibitor (NNRTI), is used to treat HIV-1 infection and AIDS.
Targets
Reverse transcriptase [1]
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 itself is an inhibitor of only CYP3A4 at concentrations that are well above those of therapeutic relevance (Ki = 270 mM). [1] 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. [2] As a dipyridodiazepinone, it 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] 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. [4]
In vivo

Nevirapine (NSC 641530) is metabolized to 4-CANVP as a major metabolite in all male animals and in 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)

References

  • https://pubmed.ncbi.nlm.nih.gov/10570031/
  • https://pubmed.ncbi.nlm.nih.gov/12747369/
  • https://pubmed.ncbi.nlm.nih.gov/1371691/
  • https://pubmed.ncbi.nlm.nih.gov/7533167/
  • https://pubmed.ncbi.nlm.nih.gov/10570025/

Customer Product Validation

Cells were inoculated with 0.05 ng mock-exposed and semen-exposed HIV, and 0.5 ng HIV as infectivity-matched control. Infection rates were measured 3 d post infection by measuring β-galactosidase. Left: the mean enzyme activities. Middle: normalized infection rates in which reporter enzyme activities obtained from infected cells in the absence of nevirapine were set at 100%. Right: IC50 values.

Data from [ , , Sci Transl Med, 2014, 6(262): 262ra157 ]

Selleck's Nevirapine (NSC 641530) Has Been Cited by 13 Publications

Inhibiting EZH2 targets atypical teratoid rhabdoid tumor by triggering viral mimicry via both RNA and DNA sensing pathways [ Nat Commun, 2024, 15(1):9321] PubMed: 39472584
Discovery of Benzisothiazolone Derivatives as Bifunctional Inhibitors of HIV-1 Reverse Transcriptase DNA Polymerase and Ribonuclease H Activities [ Biomolecules, 2024, 14(7)819] PubMed: 39062532
Biological and Structural Analyses of New Potent Allosteric Inhibitors of HIV-1 Integrase [ Antimicrob Agents Chemother, 2023, 67(7):e0046223] PubMed: 37310224
DNA ultra-sensitive quantification, a technology for studying HIV unintegrated linear DNA [ Cell Rep Methods, 2023, 3(4):100443] PubMed: 37159665
LINE-1 activation in the cerebellum drives ataxia [ Neuron, 2022, 110(20):3278-3287.e8] PubMed: 36070749
Reduction of CD8 T cell functionality but not inhibitory capacity by integrase inhibitors [ J Virol, 2022, JVI0173021] PubMed: 35019724
Unexpected similarity between HIV-1 reverse transcriptase and tumor necrosis factor binding sites revealed by computer vision [ J Cheminform, 2021, 13(1):90] PubMed: 34814950
A synthetic resveratrol analog termed Q205 reactivates latent HIV-1 through activation of P-TEFb [ Biochem Pharmacol, 2021, 197:114901] PubMed: 34971588
Limitations of dual-fluorescent HIV reporter viruses in a model of pre-activation latency. [ J Int AIDS Soc, 2019, 22(12):e25425] PubMed: 31855322
Nonnucleoside Reverse Transcriptase Inhibitor Hypersusceptibility and Resistance by Mutation of Residue 181 in HIV-1 Reverse Transcriptase. [ Antimicrob Agents Chemother, 2019, 63(8)] PubMed: 31160281

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.