WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 202103
Description: 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.
MedKoo Cat#: 202103
Name: Ostarine (MK2866)
Chemical Formula: C19H14F3N3O3
Exact Mass: 389.09873
Molecular Weight: 389.33
Elemental Analysis: C, 58.61; H, 3.62; F, 14.64; N, 10.79; O, 12.33
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
|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||Max Conc. mg/mL||Max Conc. mM|
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. 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.|
1: Girgis CM, Mokbel N, Digirolamo DJ. Therapies for musculoskeletal disease: can we treat two birds with one stone? Curr Osteoporos Rep. 2014 Jun;12(2):142-53. doi: 10.1007/s11914-014-0204-5. Review. PubMed PMID: 24633910; PubMed Central PMCID: PMC4083371.
2: Srinath R, Dobs A. Enobosarm (GTx-024, S-22): a potential treatment for cachexia. Future Oncol. 2014 Feb;10(2):187-94. doi: 10.2217/fon.13.273. PubMed PMID: 24490605.
3: Dalton JT, Taylor RP, Mohler ML, Steiner MS. Selective androgen receptor modulators for the prevention and treatment of muscle wasting associated with cancer. Curr Opin Support Palliat Care. 2013 Dec;7(4):345-51. doi: 10.1097/SPC.0000000000000015. Review. PubMed PMID: 24189892.
4: Kim J, Wang R, Veverka KA, Dalton JT. Absorption, distribution, metabolism and excretion of the novel SARM GTx-024 [(S)-N-(4-cyano-3-(trifluoromethyl)phenyl)-3-(4-cyanophenoxy)-2-hydroxy-2-methylp ropanamide] in rats. Xenobiotica. 2013 Nov;43(11):993-1009. doi: 10.3109/00498254.2013.788233. Epub 2013 Apr 22. PubMed PMID: 24074268.
5: de Rijke E, Essers ML, Rijk JC, Thevis M, Bovee TF, van Ginkel LA, Sterk SS. Selective androgen receptor modulators: in vitro and in vivo metabolism and analysis. Food Addit Contam Part A Chem Anal Control Expo Risk Assess. 2013;30(9):1517-26. doi: 10.1080/19440049.2013.810346. Epub 2013 Jul 24. PubMed PMID: 23883284.
6: Mohd Fauzi F, Koutsoukas A, Cunningham A, Gallegos A, Sedefov R, Bender A. Computer-aided (in silico) approaches in the mode-of-action analysis and safety assessment of ostarine and 4-methylamphetamine. Hum Psychopharmacol. 2013 Jul;28(4):365-78. doi: 10.1002/hup.2322. PubMed PMID: 23881885.
7: Fearon KH. Selective androgen receptor modulators in cancer cachexia? Lancet Oncol. 2013 Apr;14(4):271-2. doi: 10.1016/S1470-2045(13)70068-8. Epub 2013 Mar 14. PubMed PMID: 23499391.
8: Dobs AS, Boccia RV, Croot CC, Gabrail NY, Dalton JT, Hancock ML, Johnston MA, Steiner MS. Effects of enobosarm on muscle wasting and physical function in patients with cancer: a double-blind, randomised controlled phase 2 trial. Lancet Oncol. 2013 Apr;14(4):335-45. doi: 10.1016/S1470-2045(13)70055-X. Epub 2013 Mar 14. PubMed PMID: 23499390.
9: Gerber DE. Miscellaneous agents--cytotoxics and hormonal agents. J Thorac Oncol. 2012 Dec;7(16 Suppl 5):S387-9. doi: 10.1097/JTO.0b013e31826df198. Review. PubMed PMID: 23160328.
10: Dalton JT, Barnette KG, Bohl CE, Hancock ML, Rodriguez D, Dodson ST, Morton RA, Steiner MS. The selective androgen receptor modulator GTx-024 (enobosarm) improves lean body mass and physical function in healthy elderly men and postmenopausal women: results of a double-blind, placebo-controlled phase II trial. J Cachexia Sarcopenia Muscle. 2011 Sep;2(3):153-161. Epub 2011 Aug 2. PubMed PMID: 22031847; PubMed Central PMCID: PMC3177038.
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 ).