SR9009, also known as Stenabolic, is a research drug that was developed by professor Thomas Burris of the
Scripps Research Institute
Scripps Research, previously known as The Scripps Research Institute (TSRI), is a nonprofit American medical research facility that focuses on research and education in the biomedical sciences. Headquartered in San Diego, California, the institu ...
as an
agonist
An agonist is a chemical that activates a receptor to produce a biological response. Receptors are cellular proteins whose activation causes the cell to modify what it is currently doing. In contrast, an antagonist blocks the action of the ago ...
of
Rev-ErbA
The Rev-Erb proteins are members of the nuclear receptor (NR) superfamily of intracellular transcription factors and key regulatory components of the circadian clock. There are two forms of the receptor, Rev-Erb alpha and Rev-Erb beta, wh ...
(i.e., increases the constitutive
repression of
genes regulated by Rev-ErbA)
with a half-maximum inhibitory concentration (
IC50) = 670 nM for
Rev-ErbAα and IC
50 = 800 nM for
Rev-ErbAβ.
Activation of Rev-ErbA-α by SR9009 in mice increases exercise capacity by increasing
mitochondria
A mitochondrion (; ) is an organelle found in the Cell (biology), cells of most Eukaryotes, such as animals, plants and Fungus, fungi. Mitochondria have a double lipid bilayer, membrane structure and use aerobic respiration to generate adenosi ...
counts in
skeletal muscle
Skeletal muscles (commonly referred to as muscles) are organs of the vertebrate muscular system and typically are attached by tendons to bones of a skeleton. The muscle cells of skeletal muscles are much longer than in the other types of muscl ...
.
Abuse of SR9009 has been reported within the bodybuilding community, resulting in SR9009 being placed on the
World Anti-Doping Agency
The World Anti-Doping Agency (WADA; french: Agence mondiale antidopage, AMA) is a foundation initiated by the International Olympic Committee based in Canada to promote, coordinate, and monitor the fight against drugs in sports. The agency's key ...
list of
prohibited drugs. SR9009 and the related
SR9011
SR9011 is a research drug that was developed by Professor Thomas Burris of The Scripps Research Institute, Scripps as an agonist of Rev-ErbA alpha, Rev-ErbAα
with a half-maximum inhibitory concentration (IC50, IC50) = 790 nM for Rev-Erbα and IC ...
drug are described as "Hormone and Metabolic Modulators".
See also
*
GSK4112
GSK-4112 is an experimental drug that was developed by GlaxoSmithKline as an agonist of Rev-ErbAα. It is used for studying regulation of the circadian rhythm and its influence on diverse processes such as adipogenesis, regulation of bone densit ...
*
GW501516
GW501516 (also known as GW-501,516, GW1516, GSK-516, Cardarine, and on the black market as Endurobol) is a PPARδ receptor agonist that was invented in a collaboration between Ligand Pharmaceuticals and GlaxoSmithKline in the 1990s. It entered i ...
*
SR8278
SR-8278 is an experimental drug that was developed as an antagonist of Rev-ErbAα. It has been used to demonstrate potential applications of Rev-ErbAα antagonists in the treatment of conditions such as Duchenne muscular dystrophy and Alzheimer' ...
*
SR9011
SR9011 is a research drug that was developed by Professor Thomas Burris of The Scripps Research Institute, Scripps as an agonist of Rev-ErbA alpha, Rev-ErbAα
with a half-maximum inhibitory concentration (IC50, IC50) = 790 nM for Rev-Erbα and IC ...
References
Amines
Benzene derivatives
Experimental drugs
Thiophenes
{{pharma-stub