Ostarine | Enobosarm | | MK-2866 | GTX-024 | CAS# 841205-47-8 | Androgen receptor modulator

MedKoo Cat#: 202103 | Name: Ostarine (MK2866)

Description:

WARNING: This product is for research use only, not for human or veterinary use.

Ostarine, aslo known as Enobosarm, and MK-2866 and GTX-024, is selective androgen receptor modulator with anabolic activity. Selective androgen receptor modulator (SARM) GTx-024 is designed to work like testosterone, thus promoting and/or maintaining libido, fertility, prostate growth, and muscle growth and strength. Mimicking testosterone's action, this agent may increase lean body mass, thereby ameliorating muscle wasting in the hypermetabolic state of cancer cachexia.

Chemical Structure

Ostarine (MK2866)

CAS#841205-47-8

Theoretical Analysis

MedKoo Cat#: 202103

Name: Ostarine (MK2866)

CAS#: 841205-47-8

Chemical Formula: C19H14F3N3O3

Exact Mass: 389.0987

Molecular Weight: 389.33

Elemental Analysis: C, 58.61; H, 3.62; F, 14.64; N, 10.79; O, 12.33

Price and Availability

Size	Price	Availability
10mg	USD 55.00	Ready to ship
25mg	USD 90.00	Ready to ship
50mg	USD 150.00	Ready to ship
100mg	USD 250.00	Ready to ship
200mg	USD 350.00	Ready to ship
500mg	USD 550.00	Ready to ship
1g	USD 950.00	Ready to ship
2g	USD 1,650.00	Ready to ship
5g	USD 2,950.00	Ready to ship

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Related CAS #

No Data

Synonym

MK2866; MK 2866; MK-2866; GTX024; GTX 024; GTX-024; Ostarine; Enobosarm.

IUPAC/Chemical Name

((2S)-3-(4-cyanophenoxy)-N-[4-cyano-3-(trifluoromethyl)phenyl]-2-hydroxy-2-methylpropanamide)

InChi Key

JNGVJMBLXIUVRD-SFHVURJKSA-N

InChi Code

InChI=1S/C19H14F3N3O3/c1-18(27,11-28-15-6-2-12(9-23)3-7-15)17(26)25-14-5-4-13(10-24)16(8-14)19(20,21)22/h2-8,27H,11H2,1H3,(H,25,26)/t18-/m0/s1

SMILES Code

O=C(NC1=CC=C(C#N)C(C(F)(F)F)=C1)[C@@](C)(O)COC2=CC=C(C#N)C=C2

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO, not in water

Shelf Life

>2 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Ostarine (also known as GTx-024 and MK-2866) is an investigational selective androgen receptor modulator (SARM) from GTX, Inc for treatment of conditions such as muscle wasting and osteoporosis, formerly under development by Merck & Company. GTx and Merck had clinical development plans to evaluate Ostarine for the treatment of muscle loss in patients with COPD and for the treatment of chronic sarcopenia. They had a goal of initiating an Ostarine Phase II COPD clinical trial in the first quarter of 2010 and an Ostarine Phase IIb chronic sarcopenia clinical trial in 2010. (source: http://en.wikipedia.org/wiki/Ostarine ).

Product Data

Product Data

Certificate of Analysis

View CoA: current batch, Lot#CRB60620

QC Data

View QC data: current batch, Lot#CRB60620

Safety Data Sheet (SDS)

View Safety Data Sheet (SDS)

Instruction

View handling instruction

Biological target:

GTx-007 is a selective androgen receptor modulator (SARM) and a partial agonist with a Ki of 4 nM.

In vitro activity:

TBD

In vivo activity:

The effects of the SARM drug ostarine on postmenopausal osteoporotic bone was evaluated in a rat osteoporosis model. Low dose showed no effects. The effects of intermediate and high doses were comparable overall. Improvements were mainly seen in structural properties such as bone mineral density and bone volume density. However, the effects in femora were superior to effects in vertebrae. mRNA expression of the receptor activator of NF-κB ligand decreased after treatment, and uterine weight increased. Serum levels of phosphorus increased following ostarine treatment in intermediate and high-dose groups. Short-term treatment of osteoporotic bone with ostarine led to improvement of several microstructural bone indices. While no changes in biomechanics were observed, it is conceivable that longer treatment may also improve biomechanical properties. Further studies are needed to characterize longer time effects and side effects of ostarine in osteoporosis. Reference: J Bone Miner Metab. 2019 Mar;37(2):243-255. https://link.springer.com/article/10.1007%2Fs00774-018-0929-9

	Solvent	mg/mL	mM
Solubility
	DMSO	70.0	179.80

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 389.33 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:

1. Hoffmann DB, Komrakova M, Pflug S, von Oertzen M, Saul D, Weiser L, Walde TA, Wassmann M, Schilling AF, Lehmann W, Sehmisch S. Evaluation of ostarine as a selective androgen receptor modulator in a rat model of postmenopausal osteoporosis. J Bone Miner Metab. 2019 Mar;37(2):243-255. doi: 10.1007/s00774-018-0929-9. Epub 2018 May 21. PMID: 29785666.

In vitro protocol:

TBD

In vivo protocol:

1: Taoussi O, Bambagiotti G, Gameli PS, Daziani G, Tavoletta F, Tini A, Basile G, Lo Faro AF, Carlier J. In Vitro and In Vivo Human Metabolism of Ostarine, a Selective Androgen Receptor Modulator and Doping Agent. Int J Mol Sci. 2024 Jul 17;25(14):7807. doi: 10.3390/ijms25147807. PMID: 39063049; PMCID: PMC11277069. 2: Díaz-Salazar AJ, Espinosa-Roa A, Saldívar-Guerra E, Pérez-Isidoro R. The disordering effect of SARMs on a biomembrane model. Phys Chem Chem Phys. 2024 Jul 31;26(30):20653-20662. doi: 10.1039/d4cp01002g. PMID: 39040033. 3: Kintz P, Gheddar L. Evidence of ostarine cross-contamination via sweat in 2 athletes sharing the same neoprene hamstring sleeves. An original situation of drug transfer where the anti-doping rule violation was suspended by the sport authorities. Clin Chim Acta. 2024 Jun 1;559:119688. doi: 10.1016/j.cca.2024.119688. Epub 2024 Apr 25. PMID: 38670521. 4: Maccelli A, Borioni A, Aureli F, Gaudiano MC, Manna L, Raimondo M. A screening method for the quantitative determination of selective androgen receptor modulators (SARMs) in capsules by high resolution 19F- and 1H-NMR spectroscopy. Anal Methods. 2024 Apr 4;16(14):2135-2146. doi: 10.1039/d4ay00188e. PMID: 38517236. 5: Kintz P, Gheddar L, Garnier D. Evidence of ostarine excretion in oral fluid after a single controlled oral administration. Clin Chim Acta. 2024 Apr 15;557:117879. doi: 10.1016/j.cca.2024.117879. Epub 2024 Mar 16. PMID: 38499138. 6: Alvarez JC, Etting I, Larabi IA. Body fluid contamination in the context of an adverse analytical finding in doping: About a case involving ostarine. Clin Chim Acta. 2024 Apr 15;557:117871. doi: 10.1016/j.cca.2024.117871. Epub 2024 Mar 11. PMID: 38467244. 7: Vasilev V, Boyadjiev N, Hrischev P, Gerginska F, Delchev S, Arabadzhiyska D, Komrakova M, Boeker KO, Schilling AF, Georgieva K. Ostarine blunts the effect of endurance training on submaximal endurance in rats. Naunyn Schmiedebergs Arch Pharmacol. 2024 Mar 7. doi: 10.1007/s00210-024-03030-w. Epub ahead of print. PMID: 38451281. 8: Slíž K, Piešťanský J, Mikuš P. An Ultra-High-Performance Liquid Chromatography Coupled with Tandem Mass Spectrometry Method with Online Solid- Phase Extraction Sample Preparation for the High-Throughput and Sensitive Determination of Ostarine in Human Urine. Methods Protoc. 2024 Jan 23;7(1):10. doi: 10.3390/mps7010010. PMID: 38392684; PMCID: PMC10892632. 9: Palmieri C, Linden H, Birrell SN, Wheelwright S, Lim E, Schwartzberg LS, Dwyer AR, Hickey TE, Rugo HS, Cobb P, O'Shaughnessy JA, Johnston S, Brufsky A, Tilley WD, Overmoyer B. Activity and safety of enobosarm, a novel, oral, selective androgen receptor modulator, in androgen receptor-positive, oestrogen receptor-positive, and HER2-negative advanced breast cancer (Study G200802): a randomised, open-label, multicentre, multinational, parallel design, phase 2 trial. Lancet Oncol. 2024 Mar;25(3):317-325. doi: 10.1016/S1470-2045(24)00004-4. Epub 2024 Feb 8. Erratum in: Lancet Oncol. 2024 Apr;25(4):e137. doi: 10.1016/S1470-2045(24)00144-X. Erratum in: Lancet Oncol. 2024 Jul;25(7):e284. doi: 10.1016/S1470-2045(24)00289-4. PMID: 38342115. 10: Bohlin KP, Pohanka A, Andersson A, Villén T, Ekström L. Detection of anabolic agents including selective androgen receptor modulators in samples outside of sport. Drug Test Anal. 2024 Aug;16(8):827-834. doi: 10.1002/dta.3600. Epub 2023 Nov 20. PMID: 37986708. 11: Abdulrahman A, Mohammad Azhar K, Asif Hussain A, Ali Abdullah A, Marui IS, Mohammed Hadi G, Hanan Mamdouh A, Qamre A. Molecular docking analysis of MCL-1 inhibitors for breast cancer management. Bioinformation. 2023 Jun 30;19(6):707-712. doi: 10.6026/97320630019707. PMID: 37885779; PMCID: PMC10598365. 12: Mertens JE, Bömmer MTC, Regier MB, Gabriëls G, Pavenstädt H, Grünewald I, Horvath J, Trebicka J, Schmidt H, Schlevogt B. Liver Injury after Selective Androgen Receptor Modulator Intake: A Case Report and Review of the Literature. Z Gastroenterol. 2024 Jun;62(6):935-943. English. doi: 10.1055/a-2165-6323. Epub 2023 Oct 23. PMID: 37871633. 13: Leciejewska N, Pruszynska-Oszmalek E, Sassek M, Głowacki M, Lehmenn T, Rekas-Dudziak A, Nogowski L, Nowak KW, Kolodziejski PA. Ostarine does not enhance the metabolic effect of exercise in obese rats. J Physiol Pharmacol. 2023 Aug;74(4). doi: 10.26402/jpp.2023.4.06. Epub 2023 Oct 16. PMID: 37865959. 14: Komrakova M, Schilling AF, Lehmann W, Vasilev V, Georgieva K, Gerginska F, Boyadjiev N, Delchev S. Selective Androgen Receptor Modulators Combined with Treadmill Exercise Have No Bone Benefit in Healthy Adult Rats. Pharmaceuticals (Basel). 2023 Sep 5;16(9):1249. doi: 10.3390/ph16091249. PMID: 37765057; PMCID: PMC10536500. 15: Kintz P, Gheddar L, Ameline A. Interest of nail clipping tests to discriminate a tail end of a doping regimen from a contamination in case of challenging an adverse analytical finding: Case reports involving ostarine. Drug Test Anal. 2024 May;16(5):515-517. doi: 10.1002/dta.3577. Epub 2023 Sep 17. PMID: 37718535. 16: Roch PJ, Noisser L, Böker KO, Hoffmann DB, Schilling AF, Sehmisch S, Komrakova M. Advantage of ostarine over raloxifene and their combined treatments for muscle of estrogen-deficient rats. J Endocrinol Invest. 2024 Mar;47(3):709-720. doi: 10.1007/s40618-023-02188-z. Epub 2023 Sep 6. PMID: 37672168; PMCID: PMC10904410. 17: Leciejewska N, Pruszyńska-Oszmałek E, Nogowski L, Sassek M, Strowski MZ, Kołodziejski PA. Sex-specific cytotoxicity of ostarine in cardiomyocytes. Mol Cell Endocrinol. 2023 Nov 1;577:112037. doi: 10.1016/j.mce.2023.112037. Epub 2023 Aug 3. PMID: 37543162. 18: Böker KO, Komrakova M, Fahrendorff L, Spelsberg BR, Hoffmann DB, Schilling AF, Lehmann W, Taudien S, Sehmisch S. Treatment of osteoporosis using a selective androgen receptor modulator ostarine in an orchiectomized rat model. Endocrine. 2023 Sep;81(3):579-591. doi: 10.1007/s12020-023-03422-7. Epub 2023 Jun 28. PMID: 37378829; PMCID: PMC10403398. 19: Leciejewska N, Kołodziejski PA, Sassek M, Nogowski L, Małek E, Pruszyńska- Oszmałek E. Ostarine-Induced Myogenic Differentiation in C2C12, L6, and Rat Muscles. Int J Mol Sci. 2022 Apr 15;23(8):4404. doi: 10.3390/ijms23084404. PMID: 35457222; PMCID: PMC9031805. 20: Roch PJ, Wolgast V, Gebhardt MM, Böker KO, Hoffmann DB, Saul D, Schilling AF, Sehmisch S, Komrakova M. Combination of selective androgen and estrogen receptor modulators in orchiectomized rats. J Endocrinol Invest. 2022 Aug;45(8):1555-1568. doi: 10.1007/s40618-022-01794-7. Epub 2022 Apr 16. PMID: 35429299; PMCID: PMC9270269.