Ostarine

Catalog No.S1174 Synonyms: MK-2866, GTx-024, Enobosarm

For research use only.

Ostarine (GTx-024, MK-2866, Enobosarm) is a selective androgen receptor modulator (SARM) with Ki of 3.8 nM, and is tissue-selective for anabolic organs. Phase 3.

Ostarine Chemical Structure

CAS No. 841205-47-8

Selleck's Ostarine has been cited by 8 Publications

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Biological Activity

Description Ostarine (GTx-024, MK-2866, Enobosarm) is a selective androgen receptor modulator (SARM) with Ki of 3.8 nM, and is tissue-selective for anabolic organs. Phase 3.
Features The most potent and tissue-selective in vivo activity of SARMs to date, with favorable pharmacokinetic properties.
Targets
Androgen Receptor [1]
(Cell-free assay)
3.8 nM(Ki)
In vitro

Ostarine at the concentration of 10 nM modulates the transcriptional activity of AR in CV-1 cells cotransfected with a human AR expression vector, a luciferase reporter vector, and a control β-galactosidase vector, with 94%-100% relative activity of the transcriptional activation observed for 1 nM DHT. [1] [2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HeLa M{\PbWZ2dmO2aX;uJIF{e2G7 NXvlRW1RXHKjboPhZ5RqfmG2aX;uJI9nKGi3bXHuJIFv\HKxZ3XuJJJm[2WydH;yJJRz[W6|ZnXjeIVlKGmwIHj1cYFvKEinTHGgZ4VtdHNiYomgcJVkcW[ncnHz[UBz\XCxcoTldkBo\W6nIHHzd4F6NCCDY4Tpeol1gSB;IECuNFAyPSEQvF2u NELCV449[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Mki5O|YyOSd-MkK4PVc3OTF:L3G+
CV1 M{nZRWZ2dmO2aX;uJIF{e2G7 MYGxJJRwKDFyMECgcm0> NX7Vb2ZjSWexbnnzeEBi[3Srdnn0fUBifCC5aXzkJJR6eGViYX7kdo9o\W5icnXj[ZB1d3JiZYjwdoV{e2WmIHnuJIFnemmlYX6g[5Jm\W5ibX;ub4V6KEOYMTDj[YxteyCjc4Pld5Nm\CCjczDpcoR2[3Srb36gc4YhfHKjboPjdolxfGmxbnHsJIFkfGm4aYT5JIF1KDFidH:gNVAxOCCwTTDifUBtfWOrZnXyZZNmKHKncH;yeIVzKGenbnWgZZN{[Xl? NXjxPGY3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG1NFY2QTdpPkKxOVA3PTl5PD;hQi=>
NB1643 NIXUUplyUFSVIHHzd4F6 MkHldWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKE6EMU[0N{Bk\Wyucx?= NFTYR5U9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
OHS-50 M1PNXpFJXFNiYYPzZZk> Mn\LdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKE:KUz21NEBk\Wyucx?= MY[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
In vivo After intravenous administration of Ostarine at a single dose of 10 mg/kg, plasma concentration of Ostarine declines slowly, exhibiting a longer terminal half-life of 6.0 hours, as compared to that of other related cyano/nitro group-substituted SARMs with terminal halflives of 2.6-4.0 hours. Ostarine exhibits significantly androgenic and anabolic activity by stimulating the growth of prostate, seminal vesicles, and levator ani muscle when administered in castrated male rats; Ostarine is more potent than other cyano/nitro group-substituted SARMs. Ostarine restores the weight of the prostate to 39.2%, and seminal vesicle 78.8%, and stimulates the growth of levator ani muscle to a greater extent of 141.9% as compared with that of androgenic organs. Ostarine exhibits the highest in vivo androgenic and anabolic activity of any AR nonsteroidal agonist examined to date, with ED50 values of 0.12, 0.39 and 0.03 mg/day in prostate, seminal vesicles, and levator ani muscle, respectively, being 4 times as potent as testosterone propionate (TP) in levator ani muscle. At low dose of 0.03 mg/day, Ostarine is sufficient to exert efficacious and selective activity in anabolic tissues. [1]

Protocol (from reference)

Animal Research:[1]
  • Animal Models: Immature castrated male Sprague-Dawley rats
  • Dosages: 1 mg/day
  • Administration: Subcutaneous injection

Solubility (25°C)

In vitro

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
1% DMSO+30% polyethylene glycol+1% Tween 80
For best results, use promptly after mixing.

5 mg/mL

Chemical Information

Molecular Weight 389.33
Formula

C19H14F3N3O3

CAS No. 841205-47-8
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC(COC1=CC=C(C=C1)C#N)(C(=O)NC2=CC(=C(C=C2)C#N)C(F)(F)F)O

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

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%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04869943 Recruiting Drug: Enobosarm|Drug: Exemestane Metastatic Breast Cancer Veru Inc. October 12 2021 Phase 3
NCT03566290 Terminated Drug: GTx-024 Stress Urinary Incontinence GTx June 28 2018 Phase 2
NCT00467844 Completed Drug: GTx-024|Drug: Placebo Cachexia GTx May 2007 Phase 2

(data from https://clinicaltrials.gov, updated on 2022-11-29)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Frequently Asked Questions

Question 1:
Regarding S1174, can you tell me if this is the (L) enantiomer, (R) enantiomer or a mixture of both?

Answer:
S1174 Ostarine(MK-2866) is (S) enantiomer.

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