Choose Your Country or Region

Ostarine (GTx-024)

Name: Ostarine (GTx-024)
Brand: Selleck Chemicals
SKU: S1174
Rating: 5 (8 reviews)

Catalog No.S1174 Synonyms: MK-2866

For research use only.

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

CAS No. 841205-47-8

Selleck's Ostarine (GTx-024) has been cited by 8 Publications

Purity & Quality Control

Choose Selective Androgen Receptor Inhibitors

Related Compound Libraries

Other Androgen Receptor Products

Darolutamide (ODM-201)^New

Darolutamide (ODM-201, BAY-1841788) is a novel androgen receptor (AR) antagonist that blocks AR nuclear translocation with K_i of 11 nM. Phase 3.
Sacubitril/valsartan (LCZ696)^New

Sacubitril/valsartan (LCZ696, Sacubitril, Valsartan), consisting of valsartan and sacubitril in 1:1 molar ratio, is an orally bioavailable, dual-acting angiotensin receptor-neprilysin inhibitor (ARNi) for hypertension and heart failure. Phase 3.
Endoxifen HCl^New

Endoxifen HCl, the active metabolite of Tamoxifen, ia a potent and selective estrogen receptor antagonist. Phase 2.
Enzalutamide (MDV3100)

Enzalutamide (MDV3100) is an androgen-receptor (AR) antagonist with IC50 of 36 nM in LNCaP cells. Enzalutamide is shown to increase autophagy.
Bicalutamide (ICI-176334)

Bicalutamide (ICI-176334) is an androgen receptor (AR) antagonist with IC50 of 0.16 μM in LNCaP/AR(cs)cell line. Bicalutamide promotes autophagy.
Apalutamide (ARN-509)

Apalutamide (ARN-509) is a selective and competitive androgen receptor inhibitor with IC50 of 16 nM in a cell-free assay, useful for prostate cancer treatment. Phase 3.
Dehydroepiandrosterone (DHEA)

Dehydroepiandrosterone (DHEA, Prasterone, Dehydroisoandrosterone) is an important endogenous steroid hormone, which is an androgen receptor antagonist and an estrogen receptor agonist.
Galeterone

Galeterone (TOK-001) is a selective CYP17 inhibitor and androgen receptor (AR) antagonist with IC50 of 300 nM and 384 nM, respectively, and is a potent inhibitor of human prostate tumor growth. Phase 2.
Flutamide

Flutamide (SCH-13521) is an antiandrogen drug, with its active metablolite binding at androgen receptor with K_i values of 55 nM, and primarily used to treat prostate cancer.
Andarine

Andarine (GTx-007, S-4) is a selective non-steroidal androgen receptor (AR) agonist with K_i of 4 nM, tissue-selective for anabolic organs. Phase 3.

Download Inhibitor Catalog

Androgen Receptor Signaling Pathway Map

Biological Activity

Description

Ostarine (GTx-024, MK-2866) is a selective androgen receptor modulator (SARM) with K_i 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	NIPINItHfW6ldHnvckBie3OjeR?=		NEP4W5hVemGwc3HjeIl3[XSrb36gc4YhcHWvYX6gZY5lem:pZX6gdoVk\XC2b4KgeJJidnOoZXP0[YQhcW5iaIXtZY4hUGWOYTDj[YxteyCkeTDseYNq\mW{YYPlJJJmeG:{dHXyJIdmdmViYYPzZZktKEGldHn2bZR6KD1iMD6wNFE2KM7:TT6=	MXq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjh7N{[xNUc,OjJ6OUe2NVE9N2F-
CV1	MXPGeY5kfGmxbjDhd5NigQ>?	NG\1eFYyKHSxIEGwNFAhdk1?	MoPLRYdwdmm\|dDDhZ5Rqfmm2eTDheEB4cWymIIT5dIUh[W6mcn;n[Y4hemWlZYD0c5Ih\XiycnXzd4VlKGmwIHHmdolk[W5iZ4Ll[Y4hdW:wa3X5JGNXOSClZXzsd{Bie3Onc4Pl[EBieyCrbnT1Z5Rqd25ib3[geJJidnOlcnnweIlwdmGuIHHjeIl3cXS7IHH0JFEhfG9iMUCwNEBvVSCkeTDseYNq\mW{YYPlJJJmeG:{dHXyJIdmdmViYYPzZZk>	NIflUJc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUWwOlU6Pyd-MkG1NFY2QTd:L3G+
NB1643	NIrweHNyUFSVIHHzd4F6		NFPSSY9yUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiTlKxOlQ{KGOnbHzz	MkXLQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN\|koRjJ7NEO1NVM6RC:jPh?=
OHS-50	MmftdWhVWyCjc4PhfS=>		MXLxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhV0iVLUWwJINmdGy\|	MVm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR\|NUGzPUc,Ojl2M{WxN\|k9N2F-

Click to View More Cell Line Experimental Data

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

References

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. Click to purchase: Tween 80	5 mg/mL

Chemical Information

Molecular Weight	389.33
Formula	C₁₉H₁₄F₃N₃O₃
CAS No.	841205-47-8
Storage	3 years	-20°C	powder
Storage	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

Download Ostarine (GTx-024) SDF

In vivo Formulation Calculator (Clear solution)

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

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

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.)

% DMSO + % + % Tween 80 + % ddH₂O

%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
=	×	×

Dilution Calculator Molecular Weight Calculator

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 2022-01-17)

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

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

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.

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):