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#32519780   2020/06/10 To Up

Development of a multi-residue high-throughput UHPLC-MS/MS method for routine monitoring of SARM compounds in equine and bovine blood.

Selective androgen receptor modulators (SARMs) are a group of anabolic enhancer drugs posing threats to the integrity of animal sports and the safety of animal-derived foods. The current research describes for the first time the development of a semi-quantitative assay for the monitoring of SARM family compounds in blood and establishes the relative stability of these analytes under various storage conditions prior to analysis. The presented screening method validation was performed in line with current EU legislation for the inspection of livestock and produce of animal origin, with detection capability (CCβ) values determined at 0.5 ng/mL (Ly2452473), 1 ng/mL (AC-262536 and PF-06260414), 2 ng/mL (bicalutamide, GLPG0492, LGD-2226, ostarine, S-1, S-6, and S-23), and 5 ng/mL (andarine, BMS-564929, LGD-4033, RAD140, and S-9), respectively. The applicability of the developed assay was demonstrated through the analysis of blood samples from racehorses and cattle. The developed method presents a high-throughput cost-effective tool for the routine screening for a range of SARM compounds in sport and livestock animals.
Emiliano Ventura, Anna Gadaj, Tom Buckley, Mark H Mooney

1812 related Products with: Development of a multi-residue high-throughput UHPLC-MS/MS method for routine monitoring of SARM compounds in equine and bovine blood.

400Tests1 Set96T100 μg1 mL

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#31734960   2019/11/17 To Up

A novel approach to the quantification of urinary aryl-propionamide-derived SARMs by UHPLC-MS/MS.

A simple and sensitive procedure for the quantification of two commonly abused aryl-propionamide-derived selective androgen receptor modulators (SARMs), namely S-4 (GTx-007, andarine) and S-22 (GTx-024, MK-2866, ostarine, enobosarm), has been described. Urine samples were prepared for analysis by means of a dispersive liquid-liquid microextraction using methanol and chloroform as dispersive and extracting solvents, respectively. Factors that might influence the extraction process as well as their optimum conditions were evaluated by Box-Benken and central composite designs. After extraction, the analytes were quantified by UHPLC-MS/MS. The proposed procedure was validated on human urine samples. As a result, for both SARMs the detection limits were observed at 0.05 ng/mL and calibration curves were linear in the concentration range of 0.25-50 ng/mL with the coefficient of determination of 0.998.
Azamat Temerdashev, Ekaterina Dmitrieva, Alice Azaryan, Elina Gashimova

1654 related Products with: A novel approach to the quantification of urinary aryl-propionamide-derived SARMs by UHPLC-MS/MS.

1 module0.1 mg1 module5 g430 tests100 µg100 µg

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#31319382   // To Up

Selective androgen receptor modulators (SARMs) have specific impacts on the mouse uterus.

Selective androgen receptor modulators (SARMs) have been proposed as therapeutics for women suffering from breast cancer, muscle wasting or urinary incontinence. The androgen receptor (AR) is expressed in the uterus but the impact of SARMs on the function of this organ is unknown. We used a mouse model to compare the impact of SARMs (GTx-007/Andarine®, GTx-024/Enobosarm®), Danazol (a synthetic androstane steroid) and dihydrotestosterone (DHT) on tissue architecture, cell proliferation and gene expression. Ovariectomised mice were treated daily for 7 days with compound or vehicle control (VC). Uterine morphometric characteristics were quantified using high-throughput image analysis (StrataQuest; TissueGnostics), protein and gene expression were evaluated by immunohistochemistry and RT-qPCR, respectively. Treatment with GTx-024, Danazol or DHT induced significant increases in body weight, uterine weight and the surface area of the endometrial stromal and epithelial compartments compared to VC. Treatment with GTx-007 had no impact on these parameters. GTx-024, Danazol and DHT all significantly increased the percentage of Ki67-positive cells in the stroma, but only GTx-024 had an impact on epithelial cell proliferation. GTx-007 significantly increased uterine expression of Wnt4 and Wnt7a, whereas GTx-024 and Danazol decreased their expression. In summary, the impact of GTx-024 and Danazol on uterine cells mirrored that of DHT, whereas GTx-007 had minimal impact on the tested parameters. This study has identified endpoints that have revealed differences in the effects of SARMs on uterine tissue and provides a template for preclinical studies comparing the impact of compounds targeting the AR on endometrial function.
Ioannis Simitsidellis, Arantza Esnal-Zuffiaure, Olympia Kelepouri, Elisabeth O'Flaherty, Douglas A Gibson, Philippa T K Saunders

1213 related Products with: Selective androgen receptor modulators (SARMs) have specific impacts on the mouse uterus.

100ug100ug2 mL100 4 Membranes/Box100ug Lyophilized100 TESTS200ul25 µg4 Membranes/Box100.00 ug50 ug

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#31053351   2019/04/22 To Up

Development and validation of a semi-quantitative ultra-high performance liquid chromatography-tandem mass spectrometry method for screening of selective androgen receptor modulators in urine.

A semi-quantitative method was developed to monitor the misuse of 15 SARM compounds belonging to nine different families, in urine matrices from a range of species (equine, canine, human, bovine and murine). SARM residues were extracted from urine (200 μL) with tert-butyl methyl ether (TBME) without further clean-up and analysed by ultra-high performance liquid chromatography coupled to tandem mass spectrometry (UHPLC-MS/MS). A 12 min gradient separation was carried out on a Luna Omega Polar C18 column, employing water and methanol, both containing 0.1% acetic acid (v/v), as mobile phases. The mass spectrometer was operated both in positive and negative electrospray ionisation modes (ESI±), with acquisition in selected reaction monitoring (SRM) mode. Validation was performed according to the EU Commission Decision 2002/657/EC criteria and European Union Reference Laboratories for Residues (EU-RLs) guidelines with CCβ values determined at 1 ng mL, excluding andarine (2 ng mL) and BMS-564929 (5 ng mL), in all species. This rapid, simple and cost effective assay was employed for screening of bovine, equine, canine and human urine to determine the potential level of SARMs abuse in stock farming, competition animals as well as amateur and elite athletes, ensuring consumer safety and fair play in animal and human performance sports.
Emiliano Ventura, Anna Gadaj, Gail Monteith, Alexis Ripoche, Jim Healy, Francesco Botrè, Saskia S Sterk, Tom Buckley, Mark H Mooney

2752 related Products with: Development and validation of a semi-quantitative ultra-high performance liquid chromatography-tandem mass spectrometry method for screening of selective androgen receptor modulators in urine.

400Tests100ug2 Pieces/Box100Tests100ul100ug100ug2 Pieces/Box50 ug 50 ug 100ul200

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#30617860   2019/01/07 To Up

TiO Photocatalyzed Oxidation of Drugs Studied by Laser Ablation Electrospray Ionization Mass Spectrometry.

In drug discovery, it is important to identify phase I metabolic modifications as early as possible to screen for inactivation of drugs and/or activation of prodrugs. As the major class of reactions in phase I metabolism is oxidation reactions, oxidation of drugs with TiO photocatalysis can be used as a simple non-biological method to initially eliminate (pro)drug candidates with an undesired phase I oxidation metabolism. Analysis of reaction products is commonly achieved with mass spectrometry coupled to chromatography. However, sample throughput can be substantially increased by eliminating pretreatment steps and exploiting the potential of ambient ionization mass spectrometry (MS). Furthermore, online monitoring of reactions in a time-resolved way would identify sequential modification steps. Here, we introduce a novel (time-resolved) TiO-photocatalysis laser ablation electrospray ionization (LAESI) MS method for the analysis of drug candidates. This method was proven to be compatible with both TiO-coated glass slides as well as solutions containing suspended TiO nanoparticles, and the results were in excellent agreement with studies on biological oxidation of verapamil, buspirone, testosterone, andarine, and ostarine. Finally, a time-resolved LAESI MS setup was developed and initial results for verapamil showed excellent analytical stability for online photocatalyzed oxidation reactions within the set-up up to at least 1 h. Graphical Abstract.
Fred A M G van Geenen, Maurice C R Franssen, Ville Miikkulainen, Mikko Ritala, Han Zuilhof, Risto Kostiainen, Michel W F Nielen

1245 related Products with: TiO Photocatalyzed Oxidation of Drugs Studied by Laser Ablation Electrospray Ionization Mass Spectrometry.

1 kit(s) 100 tests100 tests 100 Slides 1 kit(s) 5 G 100 Slides 10 UG

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#29319101   // To Up

Structural elucidation of major selective androgen receptor modulator (SARM) metabolites for doping control.

Selective androgen receptor modulators (SARMs) are a class of androgen receptor drugs, which have a high potential to be performance enhancers in human and animal sports. Arylpropionamides are one of the major SARM classes and get rapidly metabolized significantly complicating simple detection of misconduct in blood or urine sample analysis. Specific drug-derived metabolites are required as references due to a short half-life of the parent compound but are generally lacking. The difficulty in metabolism studies is the determination of the correct regio and stereoselectivity during metabolic conversion processes. In this study, we have elucidated and verified the chemical structure of two major equine arylpropionamide-based SARM metabolites using a combination of chemical synthesis and liquid chromatography-mass spectrometry (LC-MS) analysis. These synthesized SARM-derived metabolites can readily be utilized as reference standards for routine mass spectrometry-based doping control analysis of at least three commonly used performance-enhancing drugs to unambigously identify misconduct.
Neeraj Garg, Annelie Hansson, Heather K Knych, Scott D Stanley, Mario Thevis, Ulf Bondesson, Mikael Hedeland, Daniel Globisch

2010 related Products with: Structural elucidation of major selective androgen receptor modulator (SARM) metabolites for doping control.

100ug1 ml100ul1000 100ug100ul100ug200ul200ug100ul100ug

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#29183075   // To Up

Chemical Composition and Labeling of Substances Marketed as Selective Androgen Receptor Modulators and Sold via the Internet.

Recent reports have described the increasing use of nonsteroidal selective androgen receptor modulators, which have not been approved by the US Food and Drug Administration (FDA), to enhance appearance and performance. The composition and purity of such products is not known.
Ryan M Van Wagoner, Amy Eichner, Shalender Bhasin, Patricia A Deuster, Daniel Eichner

2626 related Products with: Chemical Composition and Labeling of Substances Marketed as Selective Androgen Receptor Modulators and Sold via the Internet.

100ug5mg100.00 ul1 ml100ug50 ug 100ug100ul50 ug 100ul100ul100ug

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#26990774   2016/03/16 To Up

Specific characterization of non-steroidal selective androgen peceptor modulators using supercritical fluid chromatography coupled to ion-mobility mass spectrometry: application to the detection of enobosarm in bovine urine.

Currently under development for therapeutic purposes in human medicine, non-steroidal selective androgen receptor modulators (non-steroidal SARMs) are also known to impact growth associated pathways. As such, they present a potential for abuse in sports and food-producing animals as interesting alternative anabolic substances. Forbidden since 2008 by the World Anti-Doping Agency (WADA) these compounds are however easily available and could be (mis)used in livestock production as growth promoters. To prevent such practices, dedicated analytical strategies have to be developed for specific and sensitive detection of these compounds in biological matrices. Using an innovative analytical platform constituted of supercritical fluid chromatography coupled to ion mobility-mass spectrometry, the present study enabled efficient separation and identification in urine of 4 of these drugs (andarine, bicalutamide, hydroxyflutamide, and enobosarm) in accordance with European Union criteria (Commission Decision 2002/657/EC). Besides providing information about compounds structure and behaviour in gas phase, such a coupling enabled reaching low limits of detection (LOD < 0.05 ng.mL for andarine and limits of detection < 0.005 ng.mL for the three others) in urine with good repeatability (CV < 21 %). The workflow has been applied to quantitative determination of enobosarm elimination in urine of treated bovine (200 mg, oral). Copyright © 2016 John Wiley & Sons, Ltd.
Laure Beucher, Gaud Dervilly-Pinel, Nora Cesbron, Mylène Penot, Audrey Gicquiau, Fabrice Monteau, Bruno Le Bizec

2307 related Products with: Specific characterization of non-steroidal selective androgen peceptor modulators using supercritical fluid chromatography coupled to ion-mobility mass spectrometry: application to the detection of enobosarm in bovine urine.

96 wells 100ul96 wells (1 kit)100 mg101 mg

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#26969924   // To Up

Investigation of the selective androgen receptor modulators S1, S4 and S22 and their metabolites in equine plasma using high-resolution mass spectrometry.

Selective androgen receptor modulators (SARMs) are prohibited in sports due to their performance enhancing ability. It is important to investigate the metabolism to determine appropriate targets for doping control. This is the first study where the equine metabolites of SARMs S1, S4 (Andarine) and S22 (Ostarine) have been studied in plasma.
Annelie Hansson, Heather Knych, Scott Stanley, Mario Thevis, Ulf Bondesson, Mikael Hedeland

1099 related Products with: Investigation of the selective androgen receptor modulators S1, S4 and S22 and their metabolites in equine plasma using high-resolution mass spectrometry.

100ug0.1 mg200ug50 ug 200ul100ug1 ml100ul200 100ul100ug100ul

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#26456227   2015/10/12 To Up

Detection of the selective androgen receptor modulator andarine (S-4) in a routine equine blood doping control sample.


Adam T Cawley, Corrine Smart, Candace Greer, Marcus Liu Lau, John Keledjian

1089 related Products with: Detection of the selective androgen receptor modulator andarine (S-4) in a routine equine blood doping control sample.

100ul2 Pieces/Box100ug100ug100 μg4 Sample Kit100ul

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