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Efavirenz

Catalog No. T2393 CAS 154598-52-4

Synonyms: EFV, DMP 266, Sustiva, Stocrin, L-743726

Efavirenz (DMP 266) is a Human Immunodeficiency Virus 1 Non-Nucleoside Analog Reverse Transcriptase Inhibitor. The mechanism of action of efavirenz is as a Non-Nucleoside Reverse Transcriptase Inhibitor, and Cytochrome P450 3A Inducer, and Cytochrome P450 2B6 Inducer, and Cytochrome P450 2C9 Inhibitor, and Cytochrome P450 2C19 Inhibitor, and Cytochrome P450 3A4 Inhibitor. The chemical classification of efavirenz is Non-Nucleoside Analog.

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Efavirenz, CAS 154598-52-4

Pack Size	Availability	Price/USD
5 mg	In stock	$ 35.00
10 mg	In stock	$ 48.00
25 mg	In stock	$ 65.00
50 mg	In stock	$ 82.00
100 mg	In stock	$ 118.00
500 mg	In stock	$ 287.00
1 g	In stock	$ 425.00
1 mL * 10 mM (in DMSO)	In stock	$ 45.00

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Purity: 99.83%

Purity: 99.58%

Purity: 99.2%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Efavirenz (DMP 266) is a Human Immunodeficiency Virus 1 Non-Nucleoside Analog Reverse Transcriptase Inhibitor. The mechanism of action of efavirenz is as a Non-Nucleoside Reverse Transcriptase Inhibitor, and Cytochrome P450 3A Inducer, and Cytochrome P450 2B6 Inducer, and Cytochrome P450 2C9 Inhibitor, and Cytochrome P450 2C19 Inhibitor, and Cytochrome P450 3A4 Inhibitor. The chemical classification of efavirenz is Non-Nucleoside Analog.
Targets&IC50	HIV-1:2.93 nM (Ki)
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].
Kinase Assay	Recombinant RT enzymes are expressed, purified, and assessed for inhibition by Efavirenz (L-743726). Ki and Kii values are determined for each enzyme tested. The wild-type RT exhibited exclusively noncompetitive inhibition kinetics (data not shown), and, therefore, the Ki and Kii values are identical. Pure noncompetitive inhibition is not assumed for the mutant enzymes, and, hence, the values of both Ki and Kii are obtained from the linear mixed-type inhibition equation. The two- to threefold differences between the Ki and Kii values probably reflect a small contribution of competitive inhibition with the mutant RTs[1].
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)

Synonyms	EFV, DMP 266, Sustiva, Stocrin, L-743726
Molecular Weight	315.67
Formula	C14H9ClF3NO2
CAS No.	154598-52-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Methanol: 10 mM

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 63 mg/mL (199.58 mM)

References and Literature

1. Braz VA, et al. Biochemistry. 2010, 49(3):601-10. 2. Funes HA, et al. J Antimicrob Chemother. 2015, 70(8):2249-54. 3. Apostolova N, et al. J Hepatol. 2013, 59(4):780-9. 4. Caulk AW, et al. J Biomech. 2015, 48(10):2176-80. 5. Chu, Liuxi, et al. Simultaneous quantitation of zidovudine, efavirenz, lopinavir and ritonavir in human hair by liquid chromatography-atmospheric pressure chemical ionization-tandem mass spectrometry [J]. Journal of Chromatography B . 2018 Oct 15;1097-1098:54-63. 6. Zhang R, Zhang F, Sun Z, et al. LINE-1 Retrotransposition Promotes the Development and Progression of Lung Squamous Cell Carcinoma by Disrupting the Tumor Suppressor Gene FGGY[J]. Cancer research. 2019: canres. 0076.2019.

Citations

1. Cheng C, Ji Z, Sheng Y, et al. Aphthous ulcer drug inhibits prostate tumor metastasis by targeting IKKɛ/TBK1/NF-κB signaling. Theranostics. 2018, 8(17): 4633 2. Zhang R, Zhang F, Sun Z, et al. LINE-1 Retrotransposition Promotes the Development and Progression of Lung Squamous Cell Carcinoma by Disrupting the Tumor Suppressor Gene FGGY. Cancer Research. 2019: canres. 0076 3. Wu Y, Chu L, Yang H, et al. Simultaneous Determination of 6 Antiretroviral Drugs in Human Hair Using an LC-ESI+-MS/MS Method: Application to Adherence Assessment. Therapeutic Drug Monitoring. 2021, 43(6): 756-765.

Related compound libraries

This product is contained In the following compound libraries：

EMA Approved Drug Library Inhibitor Library Drug Repurposing Compound Library Anti-Cancer Drug Library Anti-Cancer Clinical Compound Library Anti-Cancer Approved Drug Library Pediatric Drug Library Drug-induced Liver Injury (DILI) Compound Library Bioactive Compounds Library Max FDA-Approved Drug Library

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Efavirenz 154598-52-4 Autophagy Microbiology/Virology Proteases/Proteasome Reverse Transcriptase HIV Protease HIV inhibit EFV DMP-266 DMP266 Human immunodeficiency virus DMP 266 L743726 L 743726 Inhibitor Sustiva Stocrin L-743726 inhibitor

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