2. Vitamin D Related/Nuclear Receptor
  3. Androgen Receptor
  4. GSK-2881078

GSK-2881078 is an orally active and nonsteroidal selective androgen receptor modulator (SARM) which act as partial AR agonists in androgenic tissues while mainly as complete AR agonists in synthetic metabolic tissues,induces AR-mediated transcriptional activation in PC3(AR)2 cells (EC50 = 3.99 nM) and the effect can be inhibited by the non-steroidal AR antagonist Bicalutamide. GSK-2881078 can be used in research of muscle weakness and cachexia associated with both chronic and acute illness.

For research use only. We do not sell to patients.

GSK-2881078 Chemical Structure

GSK-2881078 Chemical Structure

CAS No. : 1539314-06-1

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 88 In-stock
Solution
10 mM * 1 mL in DMSO USD 88 In-stock
Solid
5 mg USD 80 In-stock
10 mg USD 130 In-stock
25 mg USD 260 In-stock
50 mg USD 420 In-stock
100 mg USD 700 In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 4 publication(s) in Google Scholar

GSK-2881078 Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

GSK-2881078 is an orally active and nonsteroidal selective androgen receptor modulator (SARM) which act as partial AR agonists in androgenic tissues while mainly as complete AR agonists in synthetic metabolic tissues,induces AR-mediated transcriptional activation in PC3(AR)2 cells (EC50 = 3.99 nM) and the effect can be inhibited by the non-steroidal AR antagonist Bicalutamide. GSK-2881078 can be used in research of muscle weakness and cachexia associated with both chronic and acute illness[1][2][3][4].

In Vitro

GSK-2881078 has EC50s of 4.44 μM and 3.99 × 10−3 μM for reporter gene of androgen inducible yeast and PC3(AR)2 cells (human prostate carcinoma cell), respectively[4].
GSK-2881078 (10−5-10 μM, 24 h) stimulates reporter gene expression dose-dependently in the PC3(AR)2, increasing the relative luminescence units from 140% to 17340%[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

GSK-2881078 Related Antibodies
Clinical Trial
Molecular Weight

330.33

Formula

C14H13F3N2O2S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

N#CC1=C(C(F)(F)F)C2=C(N([C@H](C)CS(=O)(C)=O)C=C2)C=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : ≥ 33 mg/mL (99.90 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.0273 mL 15.1364 mL 30.2728 mL
5 mM 0.6055 mL 3.0273 mL 6.0546 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.74%

COA (253 KB) LCMS (269 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.0273 mL 15.1364 mL 30.2728 mL 75.6819 mL
5 mM 0.6055 mL 3.0273 mL 6.0546 mL 15.1364 mL
10 mM 0.3027 mL 1.5136 mL 3.0273 mL 7.5682 mL
15 mM 0.2018 mL 1.0091 mL 2.0182 mL 5.0455 mL
20 mM 0.1514 mL 0.7568 mL 1.5136 mL 3.7841 mL
25 mM 0.1211 mL 0.6055 mL 1.2109 mL 3.0273 mL
30 mM 0.1009 mL 0.5045 mL 1.0091 mL 2.5227 mL
40 mM 0.0757 mL 0.3784 mL 0.7568 mL 1.8920 mL
50 mM 0.0605 mL 0.3027 mL 0.6055 mL 1.5136 mL
60 mM 0.0505 mL 0.2523 mL 0.5045 mL 1.2614 mL
80 mM 0.0378 mL 0.1892 mL 0.3784 mL 0.9460 mL
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

GSK-2881078 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

GSK-28810781539314-06-1GSK2881078GSK 2881078Androgen Receptormuscle weaknessCachexiaSARMyeastPC3(AR)2Inhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Salutation

Applicant Name *

 

Email Address *

Phone Number *

 

Organization Name *

Department *

 

Requested quantity *

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
GSK-2881078
Cat. No.:
HY-100186
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

Request for HNMR Report

We have received your request and will respond to you as soon as possible.