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[1][2][3][4].

Product Specifications

CAS Number

[1539314-06-1]

UNSPSC

12352005

Hazard Statement

H301, H360

Target

Androgen Receptor

Type

Reference compound

Related Pathways

Vitamin D Related/Nuclear Receptor

Applications

Neuroscience-Neuromodulation

Field of Research

Cancer; Endocrinology; Metabolic Disease; Inflammation/Immunology; Cardiovascular Disease; Others

Assay Protocol

https://www.medchemexpress.com/GSK-2881078.html

Purity

99.42

Solubility

DMSO : ≥ 33 mg/mL

Smiles

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

Molecular Formula

C14H13F3N2O2S

Molecular Weight

330.33

Precautions

H301, H360

References & Citations

[1]Xie Y, et al. Overview of the development of selective androgen receptor modulators (SARMs) as pharmacological treatment for osteoporosis (1998-2021) . Eur J Med Chem. 2022;230:114119.|[2]Clark RV, et al. Safety, pharmacokinetics and pharmacological effects of the selective androgen receptor modulator, GSK2881078, in healthy men and postmenopausal women. Br J Clin Pharmacol. 2017 Oct;83 (10) :2179-2194.|[3]Neil D, et al. GSK2881078, a SARM, Produces Dose-Dependent Increases in Lean Mass in Healthy Older Men and Women. J Clin Endocrinol Metab. 2018;103 (9) :3215-3224.|[4]Zierau O, et al. Comparison of the three SARMs RAD-140, GLPG0492 and GSK-2881078 in two different in vitro bioassays, and in an in silico androgen receptor binding assay. J Steroid Biochem Mol Biol. 2019 May;189:81-86.