Dapivirine (TMC120)

Catalog No.S2914

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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Dapivirine (TMC120) Chemical Structure

Dapivirine (TMC120) Chemical Structure
Molecular Weight: 329.4

Validation & Quality Control

Quality Control & MSDS

Related Compound Libraries

Dapivirine (TMC120) is available in the following compound libraries:

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Product Description

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]
IC50 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]
Features

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Van Herrewege Y, et al. Antimicrob Agents Chemother, 2004, 48(1), 337-339.

[2] Fletcher P, et al. Antimicrob Agents Chemother, 2009, 53(2), 487-495.

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Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2016-06-25)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT02658227 Not yet recruiting HIV Infections International Partnership for Microbicides, Inc. February 2016 Phase 1
NCT02808949 Active, not recruiting Human Immunodeficiency Virus International Partnership for Microbicides, Inc. February 2015 Phase 1
NCT02028338 Enrolling by invitation HIV Prevention International Partnership for Microbicides, Inc.|Microbic  ...more International Partnership for Microbicides, Inc.|Microbicide Trials Network|National Institutes of Health (NIH) March 2014 Phase 2
NCT02010593 Completed Safety/PK and Adherence/Acceptability International Partnership for Microbicides, Inc.|National  ...more International Partnership for Microbicides, Inc.|National Institute of Allergy and Infectious Diseases (NIAID) December 2013 Phase 2
NCT01952561 Not yet recruiting Pharmacokinetics International Partnership for Microbicides, Inc. November 2013 Phase 1

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Chemical Information

Download Dapivirine (TMC120) SDF
Molecular Weight (MW) 329.4
Formula

C20H19N5

CAS No. 244767-67-7
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms N/A
Solubility (25°C) * In vitro DMSO 34 mg/mL (103.21 mM)
Water <1 mg/mL (<1 mM)
Ethanol <1 mg/mL (<1 mM)
* <1 mg/ml means slightly soluble or 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 Name Benzonitrile, 4-[[4-[(2,4,6-trimethylphenyl)amino]-2-pyrimidinyl]amino]-

Tech Support

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