Efavirenz

Catalog No.S4685 Batch:S468502

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Technical Data

Formula

C14H9ClF3NO2
Molecular Weight 315.67 CAS No. 154598-52-4
Solubility (25°C)* In vitro DMSO 63 mg/mL (199.57 mM)
Ethanol 63 mg/mL (199.57 mM)
Water Insoluble
* <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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description Efavirenz 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 Assay:

[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 Study:

[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

Selleck's Efavirenz has been cited by 13 publications

Chemical inhibition of DPP9 sensitizes the CARD8 inflammasome in HIV-1-infected cells [ Nat Chem Biol, 2023, 19(4):431-439] PubMed: 36357533
Biological and Structural Analyses of New Potent Allosteric Inhibitors of HIV-1 Integrase [ Antimicrob Agents Chemother, 2023, 67(7):e0046223] PubMed: 37310224
Revealing viral and cellular dynamics of HIV-1 at the single-cell level during early treatment periods [ Cell Rep Methods, 2023, 3(6):100485] PubMed: 37426753
ATAD3A oligomerization promotes neuropathology and cognitive deficits in Alzheimer's disease models [ Nat Commun, 2022, 13(1):1121] PubMed: 35236834
Memory CD4+ T cells that co-express PD1 and CTLA4 have reduced response to activating stimuli facilitating HIV latency [ Cell Rep Med, 2022, 3(10):100766] PubMed: 36198308
Unexpected similarity between HIV-1 reverse transcriptase and tumor necrosis factor binding sites revealed by computer vision [ J Cheminform, 2021, 13(1):90] PubMed: 34814950
Reverse transcriptase inhibition potentiates target therapy in BRAF-mutant melanomas: effects on cell proliferation, apoptosis, DNA-damage, ROS induction and mitochondrial membrane depolarization [ Cell Commun Signal, 2020, 18(1):150] PubMed: 32933538
Altered Gut Microbiome under Antiretroviral Therapy: Impact of Efavirenz and Zidovudine [ ACS Infect Dis, 2020, 10.1021/acsinfecdis.0c00536] PubMed: 33346662
Conformational Changes in HIV-1 Reverse Transcriptase that Facilitate Its Maturation. [ Structure, 2019, 27(10):1581-1593] PubMed: 31471129
HIV-1 Subtype C with PYxE Insertion Has Enhanced Binding of Gag-p6 to Host Cell Protein ALIX and Increased Replication Fitness. [ J Virol, 2019, 93(9)] PubMed: 30760577

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.