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

Dapivirine  (Synonyms: TMC120; R147681)

Cat. No.: HY-14266 Purity: 99.80%
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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

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 61 In-stock
Solution
10 mM * 1 mL in DMSO USD 61 In-stock
Solid
1 mg USD 28 In-stock
5 mg USD 55 In-stock
10 mg USD 90 In-stock
25 mg USD 165 In-stock
50 mg USD 250 In-stock
100 mg USD 350 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Based on 2 publication(s) in Google Scholar

Other Forms of Dapivirine:

Dapivirine Related Antibodies

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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].

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

Dapivirine Related Antibodies

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].

MedChemExpress (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.
Appearance

Solid

Color

White to off-white

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 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : ≥ 47 mg/mL (142.68 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 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

    This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

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

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.80%

COA (252 KB) LCMS (93 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.0358 mL 15.1791 mL 30.3582 mL 75.8956 mL
5 mM 0.6072 mL 3.0358 mL 6.0716 mL 15.1791 mL
10 mM 0.3036 mL 1.5179 mL 3.0358 mL 7.5896 mL
15 mM 0.2024 mL 1.0119 mL 2.0239 mL 5.0597 mL
20 mM 0.1518 mL 0.7590 mL 1.5179 mL 3.7948 mL
25 mM 0.1214 mL 0.6072 mL 1.2143 mL 3.0358 mL
30 mM 0.1012 mL 0.5060 mL 1.0119 mL 2.5299 mL
40 mM 0.0759 mL 0.3795 mL 0.7590 mL 1.8974 mL
50 mM 0.0607 mL 0.3036 mL 0.6072 mL 1.5179 mL
60 mM 0.0506 mL 0.2530 mL 0.5060 mL 1.2649 mL
80 mM 0.0379 mL 0.1897 mL 0.3795 mL 0.9487 mL
100 mM 0.0304 mL 0.1518 mL 0.3036 mL 0.7590 mL
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Dapivirine Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Dapivirine244767-67-7TMC120 R147681TMC 120TMC-120R147681R 147681R-147681HIVReverse TranscriptaseApoptosisAutophagyHuman immunodeficiency virusInhibitorinhibitorinhibit

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