1. Anti-infection
  2. HIV
    Reverse Transcriptase

Nevirapine (Synonyms: BI-RG 587; NSC 641530; NVP)

Cat. No.: HY-10570 Purity: 99.81%
Handling Instructions

Nevirapine is a non-nucleoside inhibitor of HIV-1 reverse transcriptase used to treat and prevent HIV/AIDS; with a Ki of 270 μM.

For research use only. We do not sell to patients.

Nevirapine Chemical Structure

Nevirapine Chemical Structure

CAS No. : 129618-40-2

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 66 In-stock
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Estimated Time of Arrival: December 31
10 mg USD 60 In-stock
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Estimated Time of Arrival: December 31
50 mg USD 72 In-stock
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Estimated Time of Arrival: December 31
100 mg USD 96 In-stock
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Estimated Time of Arrival: December 31
200 mg USD 108 In-stock
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Estimated Time of Arrival: December 31
500 mg   Get quote  
1 g   Get quote  

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

Nevirapine is a non-nucleoside inhibitor of HIV-1 reverse transcriptase used to treat and prevent HIV/AIDS; with a Ki of 270 μM.

IC50 & Target

Ki: 270 μM (HIV-1 reverse transcriptase)[1]

In Vitro

Nevirapine itself is an inhibitor of only CYP3A4 at concentrations that are well above those of therapeutic relevance (Ki=270 μM)[1]. Nevirapine has been used as a re-differentiation agent to treat cancers in several human cancer models. At all doses (100, 200, 350, 500 μM) tested, nevirapine significantly inhibits cell proliferation after 48 h treatment. At high dose (500 μM), nevirapine significantly increases the percentage of apoptotic cells compared with control[2]. Nevirapine is a potent and selective inhibitor (IC50=10-100 nM) of the replication of a wide variety of HIV-1 strains in several cellular assays[3].

In Vivo

Nevirapine is available for use in combination with nucleoside HIV-1 reverse transcriptase inhibitors (e.g., zidovudine, didanosine, etc.). Nevirapine has received FDA approval for use in combination with HIV-1 protease inhibitors (e.g., saquinavir, ritonavir, indinavir, etc.). In humans, nevirapine is eliminated primarily in the urine as glucuronide conjugates of 2-, 3-, 8-, and 12-hydroxynevirapine[1]. Nevirapine is completely absorbed in both sexes of mouse, rat, rabbit, monkey, and chimpanzee. Nevirapine is extensively metabolized in both sexes of all animal species studied[4]. Nevirapine (9 mg/kg, 18 mg/kg and 36 mg/kg) shows significant reduction in ulcer severity score and ulcer index as compared to the control[5]

Clinical Trial
References
Preparing Stock Solutions
Concentration Volume Mass 1 mg 5 mg 10 mg
1 mM 3.7552 mL 18.7758 mL 37.5516 mL
5 mM 0.7510 mL 3.7552 mL 7.5103 mL
10 mM 0.3755 mL 1.8776 mL 3.7552 mL
Please refer to the solubility information to select the appropriate solvent.
Cell Assay
[2]

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[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[4]

Rats: Nevirapine and [14C] Nevirapine are dissolved together in absolute ethanol and methylene chloride (1:1, v/v) with mild heating. The concentration of drug in suspension is 2 mg/mL (20 mg/kg, 26 μCi) for oral dosing to rats and 6.7 mg/mL (20.3 mg/kg, 10 μCi males, 8.9 μCi females) for intraduodenal administration to rats before bile collection. The i.v. dose is administered to rats (1.1 mg/kg, 20 μCi) as a solution in 20% ethanol/80% saline[4].

Mice: Nevirapine and [14C] Nevirapine are dissolved together in absolute ethanol and methylene chloride (1:1, v/v) with mild heating. The concentration of drug in suspension is 2 mg/mL (20 mg/kg, 2.5 μCi) with a specific activity of 5.55 μCi/mg for oral dosing to mice[4].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

266.3

Formula

C₁₅H₁₄N₄O

CAS No.

129618-40-2

SMILES

O=C1C2=C(N=CC=C2)N(C3CC3)C4=NC=CC(C)=C4N1

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

10 mM in DMSO

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Product Name:
Nevirapine
Cat. No.:
HY-10570
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