Efavirenz

Manufactured by LGC

Sourced in Canada

Efavirenz is a laboratory product used in the analysis and research of chemical compounds. It is a non-nucleoside reverse transcriptase inhibitor (NNRTI) that can be used in the study of HIV and related viral infections. The core function of Efavirenz is to serve as a research tool for scientists and researchers working in the field of virology and pharmaceutical development.

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Lab products found in correlation

8 hydroxyefavirenz, by LGC (2 mentions) 7 hydroxyefavirenz, by LGC (2 mentions) Hexobarbital, by Merck Group (1 mentions) Purelab classic uvf, by Elga LabWater (1 mentions) Whatman, by Cytiva (1 mentions) 8 14 dihydroxyefavirenz, by LGC (1 mentions) Paraxanthine, by Merck Group (1 mentions) Amprenavir, by GlaxoSmithKline (1 mentions) Lopinavir, by Abbott (1 mentions) Ritonavir, by Abbott (1 mentions) Lamivudine, by LGC (1 mentions) Tenofovir, by LGC (1 mentions) Nevirapine, by Boehringer Ingelheim (1 mentions) Atazanavir, by Bristol-Myers Squibb (1 mentions) Ultima gold scintillation fluid, by PerkinElmer (1 mentions) Ritonavir, by LGC (1 mentions) Nevirapine, by LGC (1 mentions) Diclofenac, by Merck Group (1 mentions) Ketoprofen, by Merck Group (1 mentions) Dextromethorphan, by Merck Group (1 mentions)

5 protocols using efavirenz

Quantification of Efavirenz in Breast Milk

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Reference standard of efavirenz was obtained from Toronto Research Chemicals
Inc. (North York, ON, Canada) and hexobarbital, used as an internal standard (IS),
was obtained from Sigma-Aldrich (Gillingham, Dorset, UK). LC-MS grade acetonitrile
was obtained from Fisher scientific (Loughborough, Leicestershire, UK), methanol
from VWR International (Lutterworth, Leicestershire, UK) and water was produced from
an Elga Option 4 water purifier (Elga Labwater, High Wycombe, Buckinghamshire, UK)
and was further purified to 18.2 MΩ with a Purelab Classic UVF (Elga
LabWater, High Wycombe, Buckinghamshire, UK). Whatman 903 Protein Saver cards were
obtained from Scientific Laboratory Supplies (Hessle, East Yorkshire, UK). Blank
breast milk samples were obtained (with ethics approval) from Wirral Mothers’
Milk Bank, Clatterbridge Hospital, Wirral, UK and whole blood was obtained from
drug-free healthy volunteers.

Olagunju A., Bolaji O.O., Amara A., Waitt C., Else L., Soyinka J., Adeagbo B., Adejuyigbe E., Siccardi M., Back D., Owen A, & Khoo S. (2014). Development, validation and clinical application of a novel method for the quantification of efavirenz in dried breast milk spots using LC-MS/MS. The Journal of antimicrobial chemotherapy, 70(2), 555-561.

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Quantifying Metabolic Biomarkers in Biological Samples

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Caffeine (1,3,7 TMX), 1‐methylxanthine (1 MX), 1‐methyluric acid (1 MU), 1,7‐dimethyluric acid (1,7 DMU), 5‐acetylamino‐6‐formylamino‐3‐methyluracil (AFMU), and 1,7‐dimethylxanthine (1,7 DMX) or paraxanthine and theobromine and theophylline were purchased from Sigma–Aldrich (St. Louis, MO). Efavirenz, 8‐hydroxyEfavirenz, 8,14‐dihydroxyEfavirenz, 7‐hydroxyEfavirenz, and β‐glucuronidase were purchased from Toronto Research Chemicals (North York, Ontario, Canada). All other chemicals and solvents were high‐performance liquid chromatography (HPLC) grade or the highest quality commercially available.

Metzger I.F., Dave N., Kreutz Y., Lu J.B., Galinsky R.E, & Desta Z. (2019). CYP2B6 Genotype‐Dependent Inhibition of CYP1A2 and Induction of CYP2A6 by the Antiretroviral Drug Efavirenz in Healthy Volunteers. Clinical and Translational Science, 12(6), 657-666.

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Radiolabeled Antiretroviral Compounds Protocol

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[¹⁴C]Tetraethylammonium (specific activity = 55 mCi/mmol) and [³H]efavirenz (specific activity = 5 Ci/mmol) were purchased from American Radiolabelled Chemicals (Missouri, USA). Lopinavir was a gift from Abbott (Illinois, USA). Raltegravir sodium salt was a gift from Merck (New Jersey, USA). Etravirine was a gift from Janssen (Buckinghamshire, UK). [¹⁴C]Darunavir (specific activity = 39.19 mCi/mmol), non-radiolabelled darunavir and non-radiolabelled rilpivirine were gifts from Tibotec (Mechelen Belgium). Atazanavir was a gift from Bristol-Myers Squibb (New York, USA). Nevirapine was a gift from Boehringer Ingelheim (Berkshire, UK). Ritonavir was a gift from Abbott (Illinois, USA). Tenofovir, efavirenz and lamivudine were purchased from Toronto Research Chemicals (Toronto, Canada). Amprenavir was a gift from GlaxoSmithKline (Middlesex, UK). Ultima Gold scintillation fluid was purchased from Perkin Elmer (Boston, USA). All other drugs and reagents were obtained from Sigma (Poole, UK).

Moss D.M., Liptrott N.J., Siccardi M, & Owen A. (2015). Interactions of antiretroviral drugs with the SLC22A1 (OCT1) drug transporter. Frontiers in Pharmacology, 6, 78.

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Quantification of HIV-related Compounds

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Efavirenz, 8-hydroxyEfavirenz, nevirapine, ritonavir, rifampin and 25-desacetyIrifampin were purchased from Toronto Research Chemicals Inc. (North York, Canada). β-Glucuronidase (Type H-2, from Helix pomatia) was purchased from Sigma–Aldrich (St. Louis, MO, USA). All the other chemicals and solvents were of the highest analytical grade available.

Cho D.Y., Shen J.H., Lemler S.M., Skaar T.C., Li L., Blievernicht J., Zanger U.M., Kim K.B., Shin J.G., Flockhart D.A, & Desta Z. (2015). Rifampin enhances cytochrome P450 (CYP) 2B6-mediated efavirenz 8-hydroxylation in healthy volunteers. Drug metabolism and pharmacokinetics, 31(2), 107-116.

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Hepatocyte Xenobiotic Metabolism Profiling

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Ketoprofen, zidovudine, dextromethorphan, dextrorphan, diclofenac, repaglinide, carbazeran, irinotecan, telmisartan, and quinidine were purchased from Sigma-Aldrich (St. Louis, MO, USA). Lorazepam, naloxone, 4′-hydroxydiclofenac, diclofenac-glucuronide, 3-hydroxyquinidine, 4-hydroxycarbazeran, naloxone-glucuronide, efavirenz, 7-hydroxyefavirenz, telmisartan-glucuronide, and posaconazole were purchased from Toronto Research Chemicals (Toronto, Canada). Cryopreserved hepatocyte recovery medium, William's E medium, primary hepatocyte plating supplements, primary hepatocyte maintenance supplements, and human hepatocytes (lot: Hu8264) were purchased from Thermo Fisher Scientific (Grand Island, NY, USA). Oxazepam, midazolam, and 1′-hydroxymidazolam were synthesized at F. Hoffmann-La Roche Ltd. (Basel, Switzerland). All CN Bio components (controller, docking station, and drivers) and consumables (LC-12 plates) were acquired from CN Bio Innovations (Cambridge, UK) (Fig. S1 †).

Docci L., Milani N., Ramp T., Romeo A.A., Godoy P., Franyuti D.O., Krähenbühl S., Gertz M., Galetin A., Parrott N, & Fowler S. (2022). Exploration and application of a liver-on-a-chip device in combination with modelling and simulation for quantitative drug metabolism studies. Lab on a chip, 22(6).

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