1. Anti-infection
    Apoptosis
    Autophagy
  2. HIV
    Reverse Transcriptase
    Apoptosis
    Autophagy
  3. Dapivirine

Dapivirine (Synonyms: TMC120; R147681)

Cat. No.: HY-14266 Purity: 99.94%
Handling Instructions

Dapivirine (TMC120), the prototype of diarylpyrimidines (DAPY), is an orally active and nonnucleoside reverse transcriptase inhibitor (NRTI). Dapivirine (TMC120) binds directly to HIV-1 reverse transcriptase. Dapivirine (TMC120) regulates autophagy and induced Akt, Bad and SAPK/JNK activations.

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

Dapivirine Chemical Structure

Dapivirine Chemical Structure

CAS No. : 244767-67-7

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10 mM * 1 mL in DMSO USD 99 In-stock
Estimated Time of Arrival: December 31
5 mg USD 90 In-stock
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10 mg USD 130 In-stock
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50 mg USD 290 In-stock
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100 mg USD 390 In-stock
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Based on 2 publication(s) in Google Scholar

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Description

Dapivirine (TMC120), the prototype of diarylpyrimidines (DAPY), is an orally active and nonnucleoside reverse transcriptase inhibitor (NRTI). Dapivirine (TMC120) binds directly to HIV-1 reverse transcriptase. Dapivirine (TMC120) regulates autophagy and induced Akt, Bad and SAPK/JNK activations[1][2].

In Vitro

Dapivirine (4-64 μM, 24, 48, 72, 96 and 120 hours) inhibits proliferation of glioma cells and induces apoptosis (16 μM, 12-48 h)[1].
Dapivirine (8 and 16 μM, 12 h) enhances invasion of glioma cells[1].
Dapivirine (16 μM, 12 h, 24 h and 48 h) promotes autophagy in U87 cells[1].
Dapivirine (TMC120-R147681) apparently blocks infection in the primary cultures at a 10 nM concentration, but secondary cultures revealed that a 100 nM concentration was needed to completely prevent proviral integration[3].

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

Cell Proliferation Assay[1]

Cell Line: U87 glioblastoma cells.
Concentration: 4, 8, 16 μM.
Incubation Time: 24, 48, 72, 96 and 120 hours.
Result: Inhibited proliferation of glioma cells.
IC50 was 10.73 μM.

Apoptosis Analysis[1]

Cell Line: U87 glioblastoma cells.
Concentration: 16 μM.
Incubation Time: 12h, 24h and 48h.
Result: Induced apoptosis.
Decreased caspase-3.
In Vivo

Dapivirine (16 mg/kg, once every 3 days for 12 days) exhibits potent antitumor activity in human glioblastoma models in mice[1].
Dapivirine has been shown to have a half-life in the range of 65 to 90 h[4].

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

Animal Model: U87 cells were subcutaneously injected into the nude mice[1].
Dosage: 16 mg/kg.
Administration: Once every 3 days for 12 days.
Result: Significantly decreased the tumor volumes.
A significant decrease in Ki67 (a marker for proliferating cells that is overexpressed in many cancers) staining in sections of dapivirine-treated tumors compared to tumors from vehicle-treated mice.
Clinical Trial
Molecular Weight

329.40

Formula

C₂₀H₁₉N₅

CAS No.

244767-67-7

SMILES

CC1=CC(C)=CC(C)=C1NC2=CC=NC(NC3=CC=C(C#N)C=C3)=N2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 47 mg/mL (142.68 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.0358 mL 15.1791 mL 30.3582 mL
5 mM 0.6072 mL 3.0358 mL 6.0716 mL
10 mM 0.3036 mL 1.5179 mL 3.0358 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: 2.08 mg/mL (6.31 mM); Suspended solution; Need ultrasonic

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (6.31 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

DapivirineTMC120 R147681TMC 120TMC-120R147681R 147681R-147681HIVReverse TranscriptaseApoptosisAutophagyHuman immunodeficiency virusInhibitorinhibitorinhibit

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Dapivirine
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