Nevirapine (NSC 641530)

For research use only.

Catalog No.S1742

5 publications

Nevirapine (NSC 641530) Chemical Structure

CAS No. 129618-40-2

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

Selleck's Nevirapine (NSC 641530) has been cited by 5 publications

1 Customer Review

  • 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.

    Sci Transl Med, 2014, 6(262): 262ra157 . Nevirapine (NSC 641530) purchased from Selleck.

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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 M3zPOmZ2dmO2aX;uJIF{e2G7 NFjVR2ZCdnSrdnnyZYwh[WO2aY\peJkh[WejaX7zeEBJUVZzIGLGJIlvKEOHTT3TV{Bk\WyuczDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oII\pdpV{NWmwZIXj[YQh[3m2b4DheIhq[yCnZn\lZ5Qh[nliWGTUJIF{e2G7LDDFR|UxRTFwNTDuUS=> MmjJNVgzOjJyOEi=
human MT4 cells MVvGeY5kfGmxbjDhd5NigQ>? M4TqSGFvfGm4aYLhcEBi[3Srdnn0fUBi\2GrboP0JGh2dWGwIHntcZVvd2SnZnnjbYVv[3lidnnyeZMhOSC|dXL0fZBmKENiaX7m[YN1\WRiaX6gbJVu[W5iTWS0JINmdGy|IHHzd4V{e2WmIHHzJJJm\HWldHnvckBqdiC4aYL1d{BqdmS3Y3XkJIN6fG:yYYTobYNqfHluIFXDOVA:OC5yMES4PEDPxE1? NX\XT4tIOTl7M{O3PVc>
human Jurkat E6-1 cells MXvGeY5kfGmxbjDhd5NigQ>? M3vDUlIh\GG7cx?= NInQWoZCdnSrdnnyZYwh[WO2aY\peJkh[WejaX7zeEBJUVZzIFXuek1xe2W3ZH;2bZJ2eyCrbn\lZ5Rm\CCrbjDoeY1idiCMdYLrZZQhTTZvMTDj[YxteyCjZoTldkAzKGSjeYOgZpkhdHWlaX\ldoF{\SCjc4PhfUwhUUN3ME2wMlA1KM7:TR?= M2HRVlIyPDF2N{e2
human C1866 cells MnPDR5l1d3SxeHnjbZR6KGG|c3H5 MnPBO|IhcA>? MnnRR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gR|E5PjZiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JG1VXCCjc4PhfUwhTUN3ME2wMlA1QTR|IN88US=> NUjnXphROjFzOUS5N|k>
human MT2 cells M2r5bGZ2dmO2aX;uJIF{e2G7 NX\xcJZkPCCmYYnz NX33fIE4SW62aY\pdoFtKGGldHn2bZR6KGGpYXnud5Qhf2muZDD0fZBmKEiLVkGgN2IhcW6oZXP0[YQhcW5iaIXtZY4hVVR{IHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4YheDJ2IHHueIlo\W5icILv[JVkfGmxbjDh[pRmeiB2IHThfZMh[nliRVzJV2EtKEWFNUC9NE4xPTNizszN NX[ybYYxOjB3Mke5O|I>
HeLa cells NXHReYxDTnWwY4Tpc44h[XO|YYm= MnPSRY51cX[rcnHsJIFkfGm4aYT5JIFo[Wmwc4Sge4lt\CC2eYDlJGhKXjFiaX6gTIVN[SClZXzsd{BjgSCPQVfJJIF{e2G7LDDJR|UxRTBwMEWzJO69VQ>? MVexPFY3PTV6Mx?=
293T cells M2jPTGZ2dmO2aX;uJIF{e2G7 M3jWeGlvcGmkaYTpc44hd2Zid3ns[EB1gXCnIFjJWlEhemW4ZYLz[UB1emGwc3PybZB1[XOnIHnuJFI6O1RiY3XscJMtKEmFNUC9NE4xPiEQvF2= NInyNnoyPjV{N{S4OC=>
MDCK2 cells NGrVTlZHfW6ldHnvckBie3OjeR?= NIT0NngyOCEQvF2= NEHzOmVKdmirYnn0bY9vKG:oIHj1cYFvKE2UUEKg[ZhxemW|c3XkJIlvKE2GQ1uyJINmdGy|IHHzd4V{e2WmIHHzJIlv[3KnYYPlJIlvKGmwdILhZ4VtdHWuYYKgR21HKG[udX;y[ZNk\W6lZTDheEAyOCC3TTDifUBEVU[GQTDhd5NigQ>? NV;yOJEzOTdzN{KzNVE>

... Click to View More Cell Line Experimental Data

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

Solubility (25°C)

In vitro DMSO 53 mg/mL (199.02 mM)
Water Insoluble
Ethanol 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.

Chemical Information

Molecular Weight 266.3
Formula

C15H14N4O

CAS No. 129618-40-2
Storage powder
in solvent
Synonyms N/A
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)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O
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Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

  • Mass
    Concentration
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    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and SDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

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

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

Tel: +1-832-582-8158 Ext:3

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Reverse Transcriptase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID