Efavirenz

Catalog No.S4685 Synonyms: Sustiva, Stocrin, DMP-266, DMP 266

For research use only.

Efavirenz (Sustiva, Stocrin, DMP-266) is a synthetic non-nucleoside reverse transcriptase (RT) inhibitor with antiviral activity.

Efavirenz Chemical Structure

CAS No. 154598-52-4

Selleck's Efavirenz has been cited by 9 Publications

Purity & Quality Control

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Biological Activity

Description Efavirenz (Sustiva, Stocrin, DMP-266) is a synthetic non-nucleoside reverse transcriptase (RT) inhibitor with antiviral activity.
Targets
Reverse transcriptase [1]
In vitro

Efavirenz has direct inhibitory effect on the mitochondrial respiratory function of cultured glioblastoma and differentiated neuroblastoma cell lines[2]. ER stress markers, including CHOP and GRP78 expression (both protein and mRNA), phosphorylation of eIF2a, and presence of the spliced form of XBP1 are upregulated. Efavirenz also enhances cytosolic Ca2+ content and induced morphological changes in the ER suggestive of ER stress. This response is greatly attenuated in cells with altered mitochondrial function (Rho). The effects of Efavirenz on the ER, and particularly in regard to the mitochondrial involvement, differs from those elicited by a standard pharmacological ER stressor[3].

In vivo Efavirenz leads to arterial stiffening but, for the dose and duration tested, did not lead to elevated plaque progression in ApoE(-/-) mice[4].

Protocol (from reference)

Cell Research:

[2]

  • Cell lines: human glioma U-251MG, neuroblastoma SH-SY5Y (ATCC CRL-2266) cells
  • Concentrations: 10 μM, 25μM
  • Incubation Time: 1 h
  • Method:

    The OCR(O2 consumption rate) is measured in SH-SY5Y and U-251MG cells exposed to vehicle, 10 μM efavirenz or 25 μM efavirenz for 1 h.

Animal Research:

[1]

  • Animal Models: Sprague-Dawley rats
  • Dosages: 10, 40, and 160 mg/kg(oral); 2, 5, 10, 15 mg/kg(i.v.)
  • Administration: i.v. or p.o. administration

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 315.67
Formula

C14H9ClF3NO2

CAS No. 154598-52-4
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1CC1C#CC2(C3=C(C=CC(=C3)Cl)NC(=O)O2)C(F)(F)F

In vivo Formulation Calculator (Clear solution)

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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.

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
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Molarity Calculator

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04842981 Recruiting Drug: Tocilizumab|Drug: Sarilumab Arthritis Rheumatoid|Interaction University of Southern Denmark|Odense University Hospital|Hospital of South West Jutland|King Christian X´Hospital for Rheumatic Diseases|Sygehus Lillebaelt|Odense Patient Data Explorative Network May 25 2021 Phase 1|Phase 2
NCT04840641 Completed Drug: Flucloxacillin Healthy Volunteers|Drug Drug Interaction University of Southern Denmark|SignaTope GmbH Germany March 25 2021 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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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