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MedKoo Cat#: 317773 | Name: Enoximone
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Description:

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

Enoximone is a selective phosphodiesterase III (PDE3) inhibitor with vasodilating and positive inotropic activity that does not cause changes in myocardial oxygen consumption. Enoximone prevents the degradation of cAMP by PDE, which prolongs signal transduction and its subsequent effects. It is used in patients with congestive heart failure.

Chemical Structure

Enoximone
Enoximone
CAS#77671-31-9

Theoretical Analysis

MedKoo Cat#: 317773

Name: Enoximone

CAS#: 77671-31-9

Chemical Formula: C12H12N2O2S

Exact Mass: 0.0000

Molecular Weight: 248.30

Elemental Analysis: C, 58.05; H, 4.87; N, 11.28; O, 12.89; S, 12.91

Price and Availability

Size Price Availability Quantity
25mg USD 450.00 2 Weeks
50mg USD 750.00 2 Weeks
100mg USD 1,250.00 2 Weeks
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Related CAS #
No Data
Synonym
Enoximone; Perfan; Fenoximone; Enoximona; MDL-17043; MDL17043; MDL 17043; MDL-17,043; MDL17,043; MDL 17,043; MDL-19,438; MDL19,438; MDL 19,438;
IUPAC/Chemical Name
4-methyl-5-(4-methylsulfanylbenzoyl)-1,3-dihydroimidazol-2-one
InChi Key
ZJKNESGOIKRXQY-UHFFFAOYSA-N
InChi Code
InChI=1S/C12H12N2O2S/c1-7-10(14-12(16)13-7)11(15)8-3-5-9(17-2)6-4-8/h3-6H,1-2H3,(H2,13,14,16)
SMILES Code
CC1=C(NC(=O)N1)C(=O)C2=CC=C(C=C2)SC
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

Preparing Stock Solutions

The following data is based on the product molecular weight 248.30 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.

Recalculate based on batch purity %
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
1: Nishikawa H, Goto M, Fukunishi S, Asai A, Nishiguchi S, Higuchi K. Cancer Cachexia: Its Mechanism and Clinical Significance. Int J Mol Sci. 2021 Aug 6;22(16):8491. doi: 10.3390/ijms22168491. PMID: 34445197; PMCID: PMC8395185. 2: Bedi H, Hammond C, Sanders D, Yang HM, Yoshida EM. Drug-Induced Liver Injury From Enobosarm (Ostarine), a Selective Androgen Receptor Modulator. ACG Case Rep J. 2021 Jan 7;8(1):e00518. doi: 10.14309/crj.0000000000000518. PMID: 34368386; PMCID: PMC8337042. 3: Yuan Y, Lee JS, Yost SE, Frankel PH, Ruel C, Egelston CA, Guo W, Gillece JD, Folkerts M, Reining L, Highlander SK, Robinson K, Padam S, Martinez N, Tang A, Schmolze D, Waisman J, Sedrak M, Lee PP, Mortimer J. A Phase II Clinical Trial of Pembrolizumab and Enobosarm in Patients with Androgen Receptor-Positive Metastatic Triple-Negative Breast Cancer. Oncologist. 2021 Feb;26(2):99-e217. doi: 10.1002/onco.13583. Epub 2020 Nov 24. PMID: 33141975; PMCID: PMC7873338. 4: Leciejewska N, Pruszynska-Oszmalek E, Bien J, Nogowski L, Kolodziejski PA. Effect of ostarine (enobosarm/GTX024), a selective androgen receptor modulator, on adipocyte metabolism in Wistar rats. J Physiol Pharmacol. 2019 Aug;70(4). doi: 10.26402/jpp.2019.4.04. Epub 2019 Oct 19. PMID: 31642815. 5: Crawford J, Prado CM, Johnston MA, Gralla RJ, Taylor RP, Hancock ML, Dalton JT. Study Design and Rationale for the Phase 3 Clinical Development Program of Enobosarm, a Selective Androgen Receptor Modulator, for the Prevention and Treatment of Muscle Wasting in Cancer Patients (POWER Trials). Curr Oncol Rep. 2016 Jun;18(6):37. doi: 10.1007/s11912-016-0522-0. PMID: 27138015; PMCID: PMC4853438. 6: Leung K, Yaramada P, Goyal P, Cai CX, Thung I, Hammami MB. RAD-140 Drug- Induced Liver Injury. Ochsner J. 2022 Winter;22(4):361-365. doi: 10.31486/toj.22.0005. PMID: 36561105; PMCID: PMC9753945. 7: Weinblatt D, Roy S. Drug-Induced Liver Injury Secondary to Enobosarm: A Selective Androgen Receptor Modulator. J Med Cases. 2022 May;13(5):244-248. doi: 10.14740/jmc3937. Epub 2022 May 7. PMID: 35655632; PMCID: PMC9119364. 8: Lambert CP. Should the FDA's criteria for the clinical efficacy of cachexia drugs be changed? Is Ostarine safe and effective? J Cachexia Sarcopenia Muscle. 2021 Jun;12(3):531-532. doi: 10.1002/jcsm.12695. Epub 2021 Mar 23. PMID: 33759397; PMCID: PMC8200429. 9: Thevis M, Schänzer W. Detection of SARMs in doping control analysis. Mol Cell Endocrinol. 2018 Mar 15;464:34-45. doi: 10.1016/j.mce.2017.01.040. Epub 2017 Jan 27. PMID: 28137616. 10: 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. PMID: 24490605. 11: Cesbron N, Sydor A, Penot M, Prevost S, Le Bizec B, Dervilly-Pinel G. Analytical strategies to detect enobosarm administration in bovines. Food Addit Contam Part A Chem Anal Control Expo Risk Assess. 2017 Apr;34(4):632-640. doi: 10.1080/19440049.2016.1258122. Epub 2016 Nov 28. PMID: 27827563. 12: Dubois V, Simitsidellis I, Laurent MR, Jardi F, Saunders PT, Vanderschueren D, Claessens F. Enobosarm (GTx-024) Modulates Adult Skeletal Muscle Mass Independently of the Androgen Receptor in the Satellite Cell Lineage. Endocrinology. 2015 Dec;156(12):4522-33. doi: 10.1210/en.2015-1479. Epub 2015 Sep 22. PMID: 26393303. 13: Dart DA, Kandil S, Tommasini-Ghelfi S, Serrano de Almeida G, Bevan CL, Jiang W, Westwell AD. Novel Trifluoromethylated Enobosarm Analogues with Potent Antiandrogenic Activity In Vitro and Tissue Selectivity In Vivo. Mol Cancer Ther. 2018 Sep;17(9):1846-1858. doi: 10.1158/1535-7163.MCT-18-0037. Epub 2018 Jun 12. PMID: 29895558. 14: 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. PMID: 23499390; PMCID: PMC4898053. 15: Jain R, Coss C, Whooley P, Phelps M, Owen DH. The Role of Malnutrition and Muscle Wasting in Advanced Lung Cancer. Curr Oncol Rep. 2020 May 15;22(6):54. doi: 10.1007/s11912-020-00916-9. PMID: 32409907; PMCID: PMC8717049. 16: Roch PJ, Henkies D, Carstens JC, Krischek C, Lehmann W, Komrakova M, Sehmisch S. Ostarine and Ligandrol Improve Muscle Tissue in an Ovariectomized Rat Model. Front Endocrinol (Lausanne). 2020 Sep 17;11:556581. doi: 10.3389/fendo.2020.556581. PMID: 33042018; PMCID: PMC7528560. 17: Komrakova M, Nagel J, Hoffmann DB, Lehmann W, Schilling AF, Sehmisch S. Effect of Selective Androgen Receptor Modulator Enobosarm on Bone Healing in a Rat Model for Aged Male Osteoporosis. Calcif Tissue Int. 2020 Dec;107(6):593-602. doi: 10.1007/s00223-020-00751-x. Epub 2020 Sep 2. PMID: 32876707; PMCID: PMC7593387. 18: Pertusati F, Ferla S, Bassetto M, Brancale A, Khandil S, Westwell AD, McGuigan C. A new series of bicalutamide, enzalutamide and enobosarm derivatives carrying pentafluorosulfanyl (SF5) and pentafluoroethyl (C2F5) substituents: Improved antiproliferative agents against prostate cancer. Eur J Med Chem. 2019 Oct 15;180:1-14. doi: 10.1016/j.ejmech.2019.07.001. Epub 2019 Jul 3. PMID: 31288149. 19: Kintz P, Gheddar L, Paradis C, Chinellato M, Ameline A, Raul JS, Oliva- Labadie M. Peroxisome Proliferator-Activated Receptor Delta Agonist (PPAR- δ) and Selective Androgen Receptor Modulator (SARM) Abuse: Clinical, Analytical and Biological Data in a Case Involving a Poisonous Combination of GW1516 (Cardarine) and MK2866 (Ostarine). Toxics. 2021 Oct 7;9(10):251. doi: 10.3390/toxics9100251. PMID: 34678947; PMCID: PMC8538264. 20: 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. doi: 10.1007/s13539-011-0034-6. Epub 2011 Aug 2. PMID: 22031847; PMCID: PMC3177038.

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