Dapivirine (TMC120)

Catalog No.S2914

Dapivirine (TMC120) Chemical Structure

Molecular Weight(MW): 329.4

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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In DMSO USD 190 In stock
USD 147 In stock
USD 470 In stock
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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

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 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)
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
Formula

C20H19N5

CAS No. 244767-67-7
Storage powder
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03044379 Withdrawn HIV 1 Infection International Partnership for Microbicides, Inc. September 29, 2015 Phase 1
NCT02862171 Not yet recruiting HIV Prevention International Partnership for Microbicides, Inc. August 2016 Phase 3
NCT02858037 Recruiting Human Immunodeficiency Virus International Partnership for Microbicides, Inc. August 2016 Phase 3
NCT02847286 Active, not recruiting HIV- Prevention International Partnership for Microbicides, Inc. September 2015 Phase 1
NCT02808949 Recruiting Human Immunodeficiency Virus International Partnership for Microbicides, Inc. February 2015 Phase 1
NCT02858024 Completed HIV International Partnership for Microbicides, Inc. January 2015 Phase 1

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.

Handling Instructions

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Reverse Transcriptase Signaling Pathway Map

Related Reverse Transcriptase Products

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID