Home Microbiology Reverse Transcriptase inhibitor Efavirenz For research use only.

Efavirenz

Synonyms: DMP-266

Efavirenz is a synthetic non-nucleoside reverse transcriptase (RT) inhibitor with antiviral activity.

Efavirenz Chemical Structure

Efavirenz Chemical Structure

CAS No. 154598-52-4

Purity & Quality Control

Efavirenz Related Products

Signaling Pathway

Reverse Transcriptase Signaling Pathways

Reverse Transcriptase Signaling Pathway

Biological Activity

Description Efavirenz is a synthetic non-nucleoside reverse transcriptase (RT) inhibitor with antiviral activity.
Targets
Reverse transcriptase [1]
In vitro
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].
Cell Research 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.
In Vivo
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].
Animal Research 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
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04842981 Terminated
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
Healthy Volunteers|Drug Drug Interaction
University of Southern Denmark|SignaTope GmbH Germany
 March 25 2021 Phase 1

Chemical Information & Solubility

Molecular Weight 315.67 Formula

C14H9ClF3NO2
CAS No. 154598-52-4 SDF Download Efavirenz SDF
Smiles C1CC1C#CC2(C3=C(C=CC(=C3)Cl)NC(=O)O2)C(F)(F)F
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 63 mg/mL ( (199.57 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 63 mg/mL

Water : Insoluble


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In vivo
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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.

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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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