SR9011 powder is a potent and specific synthetic REV-ERB agonist that binds to REV-ERB-α with an EC50 ~790 nM and REV-ERB-β with EC50 ~560 nM. SR9011 also has good in vivo plasma/brain exposure. The nuclear receptors REV-ERB-α and REV-ERB-β play an integral role in regulating the expression of core clock proteins, driving rhythms in activity and metabolism. SR-9011 has been demonstrated that it is specifically lethal to cancer cells and oncogene-induced senescent cells, including melanocytic naevi, and has no effect on the viability of normal cells or tissues.
02 SR9011 powder (1379686-29-9) video
03 SR9011 powder (1379686-29-9) Base Information
|Chemical name||SR9011; SR 9011; SR-9011|
|Form||A crystalline solid|
|Appearance||white to light yellow|
|Solubility||Dimethyl formamide (DMF), DMSO, Ethanol|
|Storage Condition||Dry, dark and at 0-4 degree for short term (days to weeks) or -20 degree for long term (months to years).|
|Application||SR 9011 is a synthetic REV-ERBα/β agonist with activity in vivo. It is a lead compound for a new class of cancer drugs associated with the body’s circadian clock.|
04 SR9011 powder General Description
SR9011 powder is a SARM, specifically a REV-ERB agonist that helps to boost the constitutive repressive of the genes regulated by REV-ERBβ and REV-ERBα. Just like other SARMs, it is selective, and that means it does not have any other activity besides the intended part of the body.
It is one of today’s popular SARMs with the benefits of helping improve the metabolism of the liver, skeletal muscle, and adipose tissue. As a SARM, it promises to offer the same effects as steroids but without the usual side effects and with better benefits that help users become leaner and stronger.
05 SR9011 (1379686-29-9) powder History
SR9011 powder is a research drug that was developed by Professor Thomas Burris of Scripps as an agonist of Rev-ErbAα with a half-maximum inhibitory concentration (IC50) = 790 nM for Rev-Erbα and IC50 = 560 nM for Rev-ErbAβ.
06 SR9011 (1379686-29-9) Mechanism of actio
SR9011 works by stimulating REV-ERBα and REV-ERBβ. It also restricts the activity in the suprachiasmatic nucleus clock. Furthermore, it provides a reversible inhibition to the clock’ s circadian oscillation based on a study on mice.
Based on a study, SR9011 can alter the expression of the circadian pattern of some metabolic genes in the skeletal muscle, liver, and adipose tissue. As a result of this, the body has increased energy expenditure which equals several benefits.
The target of SR 9011 is the Rev-Erbα, which affects muscle cells. By stimulating Rev-Erbα, new mitochondria are produced while macrophages work to remove defective mitochondria. Besides Rev-Erbα, SR 9011 also changes the circadian rhythm of specific metabolic processes.
By changing those processes’ circadian rhythm, SR9011 can help induce a boost in the energy used by the body, and that leads to an increase of stamina among other benefits. It makes SR9011 one of the best performance enhancers in the market today.
07 SR9011 (1379686-29-9) Application
SR9011 is a potent and specific synthetic REV-ERB agonist that binds to REV-ERB-α with an EC50 ~790 nM and REV-ERB-β with EC50 ~560 nM. It also has good in vivo plasma/brain exposure. The nuclear receptors REV-ERB-α and REV-ERB-β play an integral role in regulating the expression of core clock proteins, driving rhythms in activity and metabolism.
Administration of SR9011 alters circadian behavior and the circadian pattern of core clock gene expression in the hypothalami of mice. The circadian expression pattern of an array of metabolic genes in the liver, skeletal muscle and adipose tissue was also altered, resulting in increased energy expenditure.
Treatment of diet-induced obese mice with SR9011 decreased obesity by reducing fat mass and markedly improved dyslipidaemia and hyperglycaemia. These results indicate that synthetic REV-ERB ligands that pharmacologically target the circadian rhythm may be beneficial in the treatment of sleep disorders as well as metabolic.
08 SR9011 (1379686-29-9) More Research
SR9011 for Bioavailability
Oral bioavailability with SR-9011 is better than SR9009, however, clinical studies conducted did use injections in their animal research.
It is possible that a 30mg ml solution of DMSO could be used as a transdermal delivery system with the same benefit and bioavailability of an injection.
DMSO is a primary carrier for many transdermal drug delivery systems.
09 SR9011 (1379686-29-9) Document Download
10 SR9011 (1379686-29-9) Reference
Sulli G, Rommel A, Wang X, Kolar MJ, Puca F, Saghatelian A, Plikus MV, Verma IM, Panda S: Pharmacological activation of REV-ERBs is lethal in cancer and oncogene-induced senescence. Nature. 2018 Jan 18;553(7688):351-355. doi: 10.1038/nature25170. Epub 2018 Jan 10. [PubMed:29320480
Solt LA, Wang Y, Banerjee S, Hughes T, Kojetin DJ, Lundasen T, Shin Y, Liu J, Cameron MD, Noel R, Yoo SH, Takahashi JS, Butler AA, Kamenecka TM, Burris TP: Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists. Nature. 2012 Mar 29;485(7396):62-8. doi: 10.1038/nature11030. [PubMed:22460951]
- 01. Overview
- 02. SR9011 powder (1379686-29-9) video
- 03. SR9011 powder (1379686-29-9) Base Information
- 04. SR9011 powder General Description
- 05. SR9011 (1379686-29-9) powder History
- 06. SR9011 (1379686-29-9) Mechanism of actio
- 07. SR9011 (1379686-29-9) Application
- 08. SR9011 (1379686-29-9) More Research
- 09. SR9011 (1379686-29-9) Document Download
- 10. SR9011 (1379686-29-9) Reference