Home Microbiology Reverse Transcriptase inhibitor Dapivirine (TMC120) For research use only.

Dapivirine (TMC120)

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.

Dapivirine (TMC120) Chemical Structure

Dapivirine (TMC120) Chemical Structure

CAS: 244767-67-7

Selleck's Dapivirine (TMC120) has been cited by 11 publications

Purity & Quality Control

Batch: S291401 DMSO] 34 mg/mL] false] Water] Insoluble] false] Ethanol] Insoluble] false Purity: 100%
100

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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.
Targets
HIV reverse transcriptase [1]
24 nM
In vitro
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]
In Vivo
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]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05416021 Recruiting HIV Infections International Partnership for Microbicides Inc. August 1 2022 Phase 1
NCT03593655 Completed HIV Infections National Institute of Allergy and Infectious Diseases (NIAID) January 14 2019 Phase 2
NCT03393468 Completed HIV Infections National Institute of Allergy and Infectious Diseases (NIAID) May 10 2018 Phase 1
NCT03239483 Completed HIV Infections National Institute of Allergy and Infectious Diseases (NIAID) October 26 2017 Phase 1

Chemical lnformation & Solubility

Molecular Weight 329.4 Formula

C20H19N5
CAS No. 244767-67-7 SDF Download Dapivirine (TMC120) SDF
Smiles CC1=CC(=C(C(=C1)C)NC2=NC(=NC=C2)NC3=CC=C(C=C3)C#N)C
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 34 mg/mL ( (103.21 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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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.

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