Dapivirine

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].

Product Specifications

CAS Number

[244767-67-7]

Product Name Alternative

TMC120; R147681

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Apoptosis; Autophagy; HIV; Reverse Transcriptase

Type

Reference compound

Related Pathways

Anti-infection; Apoptosis; Autophagy

Applications

COVID-19-anti-virus

Field of Research

Infection

Assay Protocol

https://www.medchemexpress.com/Dapivirine.html

Concentration

10mM

Purity

99.80

Solubility

DMSO : ≥ 47 mg/mL

Smiles

CC1=CC(C)=CC(C)=C1NC2=CC=NC(NC3=CC=C(C#N)C=C3)=N2

Molecular Formula

C20H19N5

Molecular Weight

329.41

Precautions

H302, H315, H319, H335

References & Citations

[1]Weiwen Liu, et al. Antitumor Activity and Mechanism of a Reverse Transcriptase Inhibitor, Dapivirine, in Glioblastoma. J Cancer. 2018 Jan 1;9 (1) :117-128.|[2]Bríd Devlin, et al. Development of dapivirine vaginal ring for HIV prevention. Antiviral Res. 2013 Dec;100 Suppl:S3-8.|[3]Yven Van Herrewege, et al. In vitro evaluation of nonnucleoside reverse transcriptase inhibitors UC-781 and TMC120-R147681 as human immunodeficiency virus microbicides. Antimicrob Agents Chemother. 2004 Jan;48 (1) :337-9.|[4]Michael E Halwes, et al. Pharmacokinetic modeling of a gel-delivered dapivirine microbicide in humans. Eur J Pharm Sci. 2016 Oct 10;93:410-8.