Dapivirine (TMC120)
For research use only.
Catalog No.S2914
8 publications

CAS No. 244767-67-7
Dapivirine (TMC120) is a non-nucleoside inhibitor for HIV reverse transcriptase with IC50 of 24 nM, inhibits a broad panel of HIV-1 isolates from different classes, inclucing a wide range of NNRTI-resistant isolates. Phase 3.
Purity & Quality Control
Choose Selective Reverse Transcriptase Inhibitors
Biological Activity
Description | Dapivirine (TMC120) is a non-nucleoside inhibitor for HIV reverse transcriptase with IC50 of 24 nM, inhibits a broad panel of HIV-1 isolates from different classes, inclucing a wide range of NNRTI-resistant isolates. Phase 3. | ||
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Targets |
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In vitro |
Dapivirine prevents HIV-induced syncytium formation in the nanomolar range and shows a low cytostatic activity. Dapivirine apparently blocks HIV-1 infection in the primary cultures at a 10 nM concentration, but secondary cultures reveals that a 100 nM concentration is needed to completely prevent proviral integration. [1] Dapivirine is well tolerated by epithelial cells, T cells, macrophages, and cervical tissue explants with CC50 (50% cytotoxic concentration) of 10 μM to 20 μM. Dapivirine potently inhibits infection by both X4- and R5-utilizing HIV-1 strains with IC50 of 1.46 nM in cell-based assays. Dapivirine potently inhibits HIV-1BaL infection of human ectocervical explant tissue in a dose-dependent manner, as evaluated by the reduction in both p24 release and provirus content in cultured explants. Dapivirine inhibits the transmission of virus to permissive T cells in a dose-dependent manner, with an IC50 of 0.1 nM. Dapivirine results in significant inhibition of HIV infection when explants are challenged with virus immediately with IC90 of 100 nM. Dapivirine is also able to inhibit viral dissemination by migratory cells. [2] |
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In vivo | Dapivirine-containing gel at vaginal level inhibits cell-associated HIV infection in mice. [3] More placebo (7 of 12) than Dapivirine (3 of 24) gel users has positive vaginal swab results, with white blood cells being the most common finding. Dapivirine (0.05%) results in Cmax of 715 pg/mL, AUC of 15 ng×h/mL and T1/2 of 89.87 hours in plasma after 14 days post-dose. Mean Dapivirine (0.05%) concentrations in vaginal fluids collected at the introitus, mid vagina, and cervix are in the range of 62-265 μg/g on day 1. [4] |
Protocol
Solubility (25°C)
In vitro | DMSO | 34 mg/mL (103.21 mM) |
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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 | 329.4 |
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Formula | C20H19N5 |
CAS No. | 244767-67-7 |
Storage |
powder in solvent |
Synonyms | N/A |
Smiles | CC1=CC(=C(C(=C1)C)NC2=NC(=NC=C2)NC3=CC=C(C=C3)C#N)C |
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 | ||||
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% DMSO % % Tween 80 % ddH2O | ||||||||||
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: : mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL,)
Method for preparing in vivo formulation:Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80,mix and clarify, next add μL ddH2O,mix and clarify.
1.Please make sure the liquid is clear before adding the next solvent.
2.Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
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Molarity Calculator
Clinical Trial Information
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
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NCT03593655 | Active not recruiting | Device: Dapivirine vaginal ring|Drug: FTC/TDF | HIV Infections | National Institute of Allergy and Infectious Diseases (NIAID) | January 14 2019 | Phase 2 |
NCT03393468 | Completed | Drug: Dapivirine gel | HIV Infections | National Institute of Allergy and Infectious Diseases (NIAID) | May 10 2018 | Phase 1 |
NCT03239483 | Completed | Drug: Dapivirine gel|Drug: Placebo gel | HIV Infections | National Institute of Allergy and Infectious Diseases (NIAID) | October 26 2017 | Phase 1 |
NCT02858037 | Completed | Combination Product: Dapivirine Vaginal Ring | Human Immunodeficiency Virus | International Partnership for Microbicides Inc. | August 2016 | Phase 3 |
Tech Support
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