GSK-2881078 Overview
GSK-2881078 is a nonsteroidal selective androgen receptor modulator (SARM) originally developed by GlaxoSmithKline and characterized in the medicinal chemistry literature as a potent, orally bioavailable androgen receptor ligand. It is widely referenced in androgen receptor pharmacology research and has been used as a tool compound in studies of androgen receptor signaling and SARM structure-activity relationships.
GSK-2881078 is not approved for human or veterinary use and is supplied strictly for laboratory and analytical research purposes.
Mechanism of Action
GSK-2881078 binds to the androgen receptor ligand-binding domain and induces AR-mediated transcriptional activation. In a PC3(AR)₂ reporter cell assay, GSK-2881078 has been reported to activate AR-mediated transcription with an EC₅₀ of approximately 3.99 nM, an effect that is blocked by the AR antagonist bicalutamide.
Reported mechanistic features include:
- High-affinity binding at the androgen receptor
- Differential transcriptional output between prostate-derived cell reporter assays and yeast androgen screens, consistent with the tissue-selective profile reported across the SARM compound class
- Oral bioavailability in published preclinical pharmacokinetic studies
These properties have supported GSK-2881078’s use as a reference ligand in mechanistic androgen receptor research.
Chemical Structure
- Chemical Name: 1-[(1R)-1-methyl-2-(methylsulfonyl)ethyl]-4-(trifluoromethyl)-1H-indole-5-carbonitrile
- Synonyms: GSK2881078; GSK 2881078
- CAS Number: 1539314-06-1
- Molecular Formula: C₁₄H₁₃F₃N₂O₂S
- Molecular Weight: 330.33 g/mol
- LogP: ~2.23 (reported)
Structural Description: GSK-2881078 is a small-molecule, nonsteroidal androgen receptor ligand built on an indole-5-carbonitrile scaffold bearing a trifluoromethyl group at the 4-position and a chiral (R)-methylsulfonyl-propyl substituent at the indole nitrogen. This framework distinguishes it from steroidal androgens and from arylpropionamide-class SARMs. Structural identification and molecular data are referenced against PubChem.
Physical and Chemical Properties
- Appearance: White to off-white crystalline powder
- Solubility: Soluble in DMSO; limited aqueous solubility
- Stability: Stable under dry, cool, light-protected storage conditions
- Recommended storage: -20 °C for long-term stability
Research Focus Areas
GSK-2881078 is commonly examined in laboratory research related to:
- Androgen receptor binding and signaling pathway studies
- SARM structure-activity relationship (SAR) analysis
- Comparative androgen receptor ligand evaluation
- Analytical and reference-standard work (including LC-MS method development referenced in anti-doping analytical literature)
- In vitro metabolism and ADME studies
Research Use Disclaimer
GSK-2881078 is intended strictly for laboratory research use only (RUO). Not for human consumption, clinical use, veterinary use, or diagnostic application. All handling and use must comply with applicable laws, regulations, and institutional laboratory safety standards.
Summary
GSK-2881078 is a structurally defined nonsteroidal selective androgen receptor modulator with documented relevance in androgen receptor pharmacology and SARM SAR research. Its indole-carbonitrile scaffold and reported nanomolar AR activity make it a useful reference compound in controlled laboratory studies of androgen receptor signaling.
| CAS Number | 1539314-06-1 |
| Other Names | GSK-2881078, GSK 2881078, GSK2881078 |
| IUPAC Name | 1-[(2R)-1-methylsulfonylpropan-2-yl]-4-(trifluoromethyl)indole-5-carbonitrile |
| Molecular Formula | C₁₄H₁₃F₃N₂O₂S |
| Molecular Weight | 330.33 |
| Dry-Fill Capsule Concentration | NA |
| Liquid Concentration And Solution | 10mg/ml (DMSO, PEG400) |
| Aliquot Concentration And Solution | NA |
