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Background And Receptor Pharmacology — Deep Dive

By Editorial Desk · published 2026-01-17 · last reviewed 2026-02-04 · Faq

This is a working overview of REV-ERB agonist, written for readers who want more than a one-paragraph summary but less than a textbook.

Reviewed 2026-02-04. Anything still debated is marked as such rather than presented as settled.

Background and Receptor Pharmacology

SR9009 is a synthetic small molecule studied as an agonist of the nuclear receptors REV-ERBα and REV-ERBβ. These receptors help regulate circadian rhythms, lipid metabolism, and inflammatory gene expression. In cell and animal experiments, SR9009 alters transcription of clock-controlled genes and metabolic pathways. The compound is not a hormone and does not resemble classical steroid structures. Its activity depends on binding to the ligand-binding domain of REV-ERB, where it can modify corepressor recruitment.

Research interest in SR9009 grew from studies of circadian biology and metabolic disease. Preclinical reports describe effects on exercise capacity, muscle metabolism, and blood lipid levels in rodents, but these findings come from controlled laboratory settings. The compound has low oral bioavailability in animals, which limits systemic exposure after swallowing. Investigators often use injected routes in experiments to achieve measurable plasma concentrations. Human clinical data are sparse, no approved therapeutic product exists, and whether animal effects translate to humans remains an open question.

Handling, Analysis, and Regulation

Analytical identification and purity assessment often use high-performance liquid chromatography with ultraviolet detection or mass spectrometry. Liquid chromatography–tandem mass spectrometry is used to detect and quantify SR9009 in biological matrices, including urine and blood, for anti-doping or pharmacokinetic studies. Nuclear magnetic resonance spectroscopy can confirm molecular structure. Stability depends on form and storage: the solid is generally more stable than solutions, and repeated freeze–thaw cycles may degrade samples. Purity is typically reported as a percentage from a certificate of analysis.

Regulatory treatment of SR9009 varies by country and context. It is not approved as a therapeutic drug by agencies such as the United States Food and Drug Administration or the European Medicines Agency. Sports authorities list it as a prohibited substance; the World Anti-Doping Agency classifies it among hormone and metabolic modulators. Legal status for personal possession or sale differs across jurisdictions, and some countries may restrict it under analog or research chemical laws. Buyers who seek verified material often rely on independent laboratory testing because online product labels may not match contents.

Sr9009 at a glance

PropertyValueNotes
Chemical classSynthetic REV-ERB agonistBinds REV-ERBα and REV-ERBβ in preclinical models
Molecular formulaC20H24ClN3O4SReported for the parent compound
CAS Registry Number1379686-30-2Common identifier in chemical databases
AppearanceOff-white to pale yellow solidTypical research chemical solid
SolubilitySoluble in DMSO and ethanol; low in waterClass: small organic molecule

Analytical Detection and Laboratory Handling

In laboratory settings, SR9009 is typically characterized by liquid chromatography–mass spectrometry (LC-MS) or high-performance liquid chromatography with ultraviolet detection (HPLC-UV). These methods can confirm identity and estimate purity, but they require reference standards for accurate quantification. Because SR9009 is not a licensed pharmaceutical, no harmonized pharmacopeial monograph exists. Laboratories often validate in-house methods for matrices such as plasma, urine, or cell culture media. Sample preparation may involve protein precipitation or liquid-liquid extraction before analysis.

Physicochemical behavior influences handling. SR9009 is described as a solid with limited aqueous solubility, so organic solvents such as dimethyl sulfoxide or ethanol are common in research stock solutions. Aqueous dilution can produce precipitates if the organic content is too low. Light, heat, and repeated freeze-thaw cycles may affect stability. Storage recommendations usually specify a desiccated freezer environment protected from light, but exact stability data depend on the formulation and matrix.

Detection in biological samples can be complicated by rapid metabolism and low circulating concentrations. Some studies report phase I and phase II metabolites, and analytical methods may need to target those species in addition to the parent compound. Immunoassays are not broadly available, so mass spectrometry remains the main confirmatory approach. For anti-doping testing, laboratories look for SR9009 and its metabolites using validated LC-MS methods. Open questions include how long metabolites remain detectable and how different routes of administration alter detection windows.

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Analytical Detection and Stability

Stability depends on physical form, temperature, light exposure, and solvent. Solid SR9009 is generally stored cold and dry, with protection from light to limit degradation. Dimethyl sulfoxide stocks are common for laboratory work, but repeated freeze-thaw cycles can reduce compound integrity. Aqueous solutions may be less stable than organic stocks, and the ethyl ester in the structure can be susceptible to hydrolysis under certain conditions. Researchers typically validate storage conditions and recheck purity before quantitative experiments, especially when using archived material.

Regulatory treatment of SR9009 varies by country and region. It is not approved as a pharmaceutical, and several jurisdictions restrict its sale for human consumption. Some authorities classify it as a research chemical, a prescription-only substance, or a prohibited performance-enhancing agent in sport. Purchasers may encounter certificates of analysis, but these documents do not guarantee identity, purity, or legality. In research settings, institutional safety reviews and controlled procurement help ensure that materials are handled under appropriate oversight. The absence of harmonized rules means that legal status can change and requires verification.

Analytical identification of SR9009 typically relies on liquid chromatography coupled with tandem mass spectrometry. In biological samples, researchers first separate the compound from matrix components using protein precipitation, liquid-liquid extraction, or solid-phase extraction. High-performance liquid chromatography with ultraviolet detection and nuclear magnetic resonance spectroscopy can support structural confirmation of reference materials. Because SR9009 is a small, relatively lipophilic molecule, reverse-phase columns and acidic mobile phases are common. Laboratories often include isotope-labeled internal standards to improve quantification and to correct for ion suppression.

Notes from published material

Headaches Enlargement of the hands, feet, nose, lips, and ears, and a general thickening of the skin Soft tissue swelling of internal organs, notably the heart with the attendant weakening of its muscularity, and the kidneys, also the vocal cords resulting in a characteristic thick, deep voice and slowing of speech Generalized expansion of the skull at the fontanelle Pronounced brow protrusion, often with ocular distension (frontal bossing) Pronounced lower jaw protrusion (prognathism) with attendant macroglossia (enlargement of the tongue) and teeth spacing Hypertrichosis, hyperpigmentation and hyperhidrosis Skin tags Carpal tunnel syndrome

ISBN 0-451-23706-4 OCLC 741538553 Megellas, James. All the Way to Berlin: A Paratrooper at War in Europe. New York: Ballantine Books, 2003. ISBN 0-89141-784-2 OCLC 50810144 Mrozek, Steven J. 82nd Airborne Division. Paducah, Ky: Turner Pub. Co, 1997. ISBN 1-56311-364-3 OCLC 52963023 Nordyke, Phil. All American, All the Way: The Combat History of the 82nd Airborne Division in World War II. St. Paul, MN: Zenith Press, 2005. ISBN 0-7603-2201-5 OCLC 60757547 Nordyke, Phil. The All Americans in World War II: A Photographic History of the 82nd Airborne Division at War. St. Paul, MN: Zenith Press, 2006. ISBN 0-7603-2617-7 OCLC 64961665 Pushies, Fred (2008). 82nd Airborne. Military Power. Minneapolis, Minnesota: Zenith Press. p. 128. ISBN 978-0-7603-3465-2. OCLC 199464749. Ruggero, Ed. Combat Jump: The Young Men Who Led the Assault into Fortress Europe, July 1943. New York: HarperCollins, 2003. ISBN 0-06-008875-3 OCLC 51978036 Saunders, Tim. Nijmegen, Grave, and Groesbeek. Barnsley, South Yorkshire: Leo Cooper, 2001. ISBN 0-85052-815-1 OCLC 49594764 Thompson, Leroy. The All Americans: The 82nd Airborne. Newton Abbot, Devon: David & Charles Publishers, 1988. ISBN 0-7153-9182-8 OCLC 19393819 Zinsmeister, Karl. Boots on the Ground: A Month with the 82nd Airborne in the Battle for Iraq. New York: Truman Talley Books/St. Martin's Press, 2003. ISBN 0-312-32663-7 OCLC 52775207 Zinsmeister, Karl, Dan Jurgens, and Raul Trevino. Combat Zone: True Tales of GIs in Iraq. New York, NY: Marvel Comics, 2005. ISBN 0-7851-1516-1 OCLC 61373604

A U.S. court rejected the lawsuit blaming UCC for causing soil and water pollution around the site of the plant and ruled that responsibility for remedial measures or related claims rested with the State Government and not with UCC. In 2005, the state government invited various Indian architects to enter their "concept for development of a memorial complex for Bhopal gas tragedy victims at the site of Union Carbide". In 2011, a conference was held on the site, with participants from European universities which was aimed for the same.

==== Distribution ==== The volume of distribution of THC is large and is approximately 10 L/kg (range 4–14 L/kg), which is due to its high lipid solubility. The plasma protein binding of THC and its metabolites is approximately 95 to 99%, with THC bound mainly to lipoproteins and to a lesser extent albumin. THC is rapidly distributed into well-vascularized organs such as lung, heart, brain, and liver, and is subsequently equilibrated into less vascularized tissue. It is extensively distributed into and sequestered by fat tissue due to its high lipid solubility, from which it is slowly released. THC is able to cross the placenta and is excreted in human breast milk.

Sources: en.wikipedia.org

Further detail

Compound 22 is a low-potency and non-selective trace amine-associated receptor 1 (TAAR1) antagonist that was identified in 2015 and was further studied in animals in 2018. The drug enhances the firing rates of dopaminergic neurons ex vivo and potentiates psychostimulant-induced hyperlocomotion and stereotypy in rodents in vivo. The latter effects are partially or fully independent of the TAAR1 however, with the mechanisms underlying these effects being unknown. Compound 22, along with EPPTB and RTI-7470-44, is one of the only TAAR1 antagonists that has been identified as of 2022.

=== Psychiatry === Suvorexant has been studied in the treatment of insomnia in people with psychiatric disorders such as depression and anxiety. It was reported to improve psychiatric symptoms and to decrease cortisol levels in these individuals. A phase IV clinical trial of suvorexant as an adjunct to antidepressant therapy in people with major depressive disorder and residual insomnia was underway as of 2019. Although orexin receptor antagonists including suvorexant could be useful for treatment of depression and anxiety, there is also indication that they could have harmful effects in these conditions (e.g., animal studies and suicidal ideation in clinical trials). More clinical research is needed to determine the place of orexin receptor antagonists in the treatment of people with depression and anxiety. There is interest in suvorexant and other orexin receptor antagonists in the potential treatment of substance use disorders, including alcohol use disorder, cocaine use disorder, and opioid use disorder.

== Etymology == The term comes from French coup d'État, literally meaning a 'stroke of state' or 'blow of state'. In French, the word État (French: [eta]) is capitalized when it denotes a sovereign political entity. One early use within text translated from French was in 1785 in a printed translation of a letter from a French merchant, commenting on an arbitrary decree, or arrêt, issued by the French king restricting the import of British wool. In the British press, the phrase came to be used to describe the various murders by Napoleon's alleged secret police, the Gens d'Armes d'Elite, who executed the Duke of Enghien: "the actors in torture, the distributors of the poisoning draughts, and the secret executioners of those unfortunate individuals or families, whom Bonaparte's measures of safety require to remove. In what revolutionary tyrants call grand[s] coups d'état, as butchering, or poisoning, or drowning, en masse, they are exclusively employed."

Sources: en.wikipedia.org

Background from the literature

=== Variable volume reactions === In some reactions the reactants and the products have significantly different densities. Consequently, as the reaction proceeds the volume of the reaction changes. This variable volume adds terms to the design equations. Taking this volume change into consideration the volume of the reaction becomes:

=== Product production === Fermentation plays a significant role in producing precursor polymers to products and food additives such as amino acids, organic acids, triglycerides and fatty acids. Amino acids are industrially produced through fermentation by microorganisms such as Corynebacterium glutamicum and Escherichia coli. The global market application for amino acids is primarily food and feed additive. L-glutamic acid and L-lysine are the most commonly found amino acids in this market with L-glutamic acid being mainly used as a food flavoring in the form of monosodium glutamate (MSG) and L-lysine being mainly used as an animal feed supplement. Other amino acids like L-threonine and L-phenylalanine are also produced on large scales for different applications. Organic acids such as citric acid, lactic acid, and acetic acid are procured by microbial fermentation. Citric acid finds widespread use in the food industry as a preservative and flavoring agent. Lactic acid is used in food preservation and as a precursor for biodegradable plastics. Acetic acid is used in food as vinegar and as a chemical reagent in industries. These organic acids are produced using microorganisms like Aspergillus niger and Lactobacillus species under controlled fermentation conditions. Fatty acids and triglycerides are produced by fermentation on oleaginous microorganisms such as Yarrowia lipolytica and certain fungi. These microorganisms can accumulate lipids under specific culture conditions and therefore are suitable for industrial-scale production of lipids.

This definition is much more practical, but an equilibrium constant defined in terms of concentrations is dependent on conditions. In particular, equilibrium constants for species in aqueous solution are dependent on ionic strength, as the quotient of activity coefficients varies with the ionic strength of the solution. The values of the standard free energy change and of the equilibrium constant are temperature dependent. To a first approximation, the van 't Hoff equation may be used.

==== European Union ==== The European Food Safety Authority (EFSA) in 2016 reviewed the current evidence, finding the relationship between serum 25(OH)D concentration and musculoskeletal health outcomes is widely variable. They considered that average requirements and population reference intake values for vitamin D cannot be derived and that a serum 25(OH)D concentration of 50 nmol/L was a suitable target value. For all people over the age of 1, including women who are pregnant or lactating, they set an adequate intake of 15 μg/day (600 IU). On the other hand, the EU Commission defined nutrition labelling for foodstuffs as regards recommended daily allowances (RDA) for vitamin D to 5 μg/day (200 IU) as 100%. The EFSA reviewed safe levels of intake in 2012, setting the tolerable upper limit for adults at 100 μg/day (4000 IU), a similar conclusion as the IOM. The Swedish National Food Agency recommends a daily intake of 10 μg (400 IU) of vitamin D3 for children and adults up to 75 years, and 20 μg (800 IU) for adults 75 and older. Non-government organisations in Europe have made their own recommendations. The German Society for Nutrition recommends 20 μg. The European Menopause and Andropause Society recommends postmenopausal women consume 15 μg (600 IU) until age 70, and 20 μg (800 IU) from age 71. This dose should be increased to 100 μg (4,000 IU) in some patients with very low vitamin D status or in case of co-morbid conditions.

Sources: en.wikipedia.org

Frequently asked questions

What is SR9009?

SR9009 is a synthetic small molecule studied as an agonist of the REV-ERB nuclear receptors. It is not an approved medicine, and its effects in humans are not well characterized.

Is SR9009 a hormone?

No. It is a synthetic ligand that binds nuclear receptors, not a steroid or peptide hormone. Its activity depends on receptor binding rather than endocrine secretion.

What is known about human use?

Clinical evidence is limited. Most published data come from cell and animal experiments. Human safety and efficacy remain uncertain.

Is SR9009 legal to buy?

Legality depends on the country and the intended use. In many places it is sold as a research chemical, but sports and medicine regulations restrict it.

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