For research use only. Not for therapeutic Use.
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].
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].
| Catalog Number | I001937 |
| CAS Number | 1539314-06-1 |
| Synonyms | 1-[(2R)-1-methylsulfonylpropan-2-yl]-4-(trifluoromethyl)indole-5-carbonitrile |
| Molecular Formula | C14H13F3N2O2S |
| Purity | ≥95% |
| InChI | InChI=1S/C14H13F3N2O2S/c1-9(8-22(2,20)21)19-6-5-11-12(19)4-3-10(7-18)13(11)14(15,16)17/h3-6,9H,8H2,1-2H3/t9-/m1/s1 |
| InChIKey | SKDVMPZQJMZEAC-SECBINFHSA-N |
| SMILES | CC(CS(=O)(=O)C)N1C=CC2=C1C=CC(=C2C(F)(F)F)C#N |
| Reference | [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. |
