Efavirenz

SKU: orb1305550

Description

Efavirenz is a non-nucleoside reverse transcriptase inhibitor (NNRTI) used in HIV-1 research. It potently inhibits viral replication in vitro and is widely employed to study antiretroviral mechanisms, drug resistance, and complex cytochrome P450-mediated metabolic interactions.

Research Area

Cell Biology, Infectious Disease & Virology, Metabolism Research, Protein Biochemistry

Key Properties

• CAS Number: 154598-52-4
• MW: 315.67
• Purity: 99.84% (May vary between batches)
• Formula: C₁₄H₉ClF₃NO₂
• SMILES: C(#CC1CC1)[C@@]2(C(F)(F)F)C=3C(NC(=O)O2)=CC=C(Cl)C3
• Target: Autophagy,HIV Protease,Parasite,Reverse Transcriptase,Endogenous Metabolite
• Solubility: Methanol:10 mM;H2O:< 1 mg/mL (insoluble or slightly soluble);DMSO:250 mg/mL (791.97 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (6.34 mM)

Bioactivity

• Target IC50:
  HIV-1:2.93 nM (Ki)
• In Vivo:
  Efavirenz leads to arterial stiffening but, for the dose and duration tested, did not lead to elevated plaque progression in ApoE(-/-) mice.
• In Vitro:
  Efavirenz has direct inhibitory effect on the mitochondrial respiratory function of cultured glioblastoma and differentiated neuroblastoma cell lines. 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.
• Cell Research:
  The OCR(O2 consumption rate) is measured in SH-SY5Y and U-251 mg cells exposed to vehicle, 10 μM efavirenz or 25 μM efavirenz for 1 h. (Only for Reference)

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

EFV, Efavirenz, L743726, L-743726, HIVProtease, HIV-1 RT, HIV Protease, HIV, Inhibitor, Human immunodeficiency virus, L 743726, inhibit, Autophagy, DMP 266, DMP266, DMP-266, ReverseTranscriptase, Reverse Transcriptase, Stocrin, Sustiva

Compound Identifiers

PubChem CID

64139