Home Proteases HIV Protease inhibitor - COVID-19 inhibitor Darunavir Ethanolate For research use only.

Darunavir Ethanolate

Synonyms: TMC-114, UIC 94017

Darunavir Ethanolate (TMC-114, UIC 94017) is a nonpeptidic HIV protease inhibitor, used to treat HIV infection.

Darunavir Ethanolate Chemical Structure

Darunavir Ethanolate Chemical Structure

CAS: 635728-49-3

Selleck's Darunavir Ethanolate has been cited by 8 Publications

1 Customer Review

Purity & Quality Control

Batch: Purity: 99.92%
99.92

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Biological Activity

Description Darunavir Ethanolate (TMC-114, UIC 94017) is a nonpeptidic HIV protease inhibitor, used to treat HIV infection.
Targets
HIV protease [1]
In vitro
In vitro Darunavir displays potent activity against HIV strains resistant to other available protease inhibitor. Darunavir inhibits P-glycoprotein-mediated efflux of calcein-acetoxymethyl ester in L-MDR1 cells with the inhibitory potency of 121 mM. [1] Darunavir is a protein inhibits that mimics the phenylalanine sequences at positions 167 and 168 of the gag-pol polypeptide and binds to the active sites of the HIV protease, thereby inhibiting its activity. Darunavir blocks the infectivity and replication of each of the HIV-1 variants at concentrations up to 5 μM. Darunavir shows strong ARV activity against a selected panel of 19 recombinant clinical isolates carrying multiple protease mutations conferring resistance to an average of five other protien inhibitors. Darunavir inhibits 75% of 1501 PI-resistant viruses tested with a half maximal effective concentration (EC50) of < 10 nM. [2]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06139796 Not yet recruiting HIV Infections PENTA Foundation|AMS-PHPT Research Collaboration|Institut National de la Santé Et de la Recherche Médicale France|Centre Mère et Enfant de la Fondation Chantal Biya|Centre Hospitalier National d''Enfants Albert Royer|University of Zimbabwe Clinical Research Centre (UZCRC)|Baylor College of Medicine June 2024 Phase 1|Phase 2
NCT05197075 Completed Human Immunodeficiency Virus (HIV) Janssen Research & Development LLC August 3 2022 Phase 1
NCT05378906 Completed Healthy Janssen Research & Development LLC June 7 2022 Phase 1

Chemical lnformation & Solubility

Molecular Weight 593.73 Formula

C27H37N3O7S.C2H5OH
CAS No. 635728-49-3 SDF Download Darunavir Ethanolate SDF
Smiles CCO.CC(C)CN(CC(C(CC1=CC=CC=C1)NC(=O)OC2COC3C2CCO3)O)S(=O)(=O)C4=CC=C(C=C4)N
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 100 mg/mL ( (168.42 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
Batch:

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In vivo Formulation Calculator

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In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

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.

Note: 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.

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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