SR9011
Synonyms:Ethyl-3-(((4-chlorobenzyl)((5-nitrothiophen-2-yl)methyl)amino)methyl)pyrrolidine-1-carboxylate
CAS No.: 1379686-30-2
Molecular formular: C20H24ClN3O4S
Molecular Weight: 437.94
Appearance: White powder
Purity: 99%
Application: SR9011 increase exercise endurance and loss weight.
Usage:reduce mass fat
Packing:1kg/foil bag
Hjtc (Xiamen) Industry Co., Ltd.
Xiamen Huayongjian Biotechnology Co., Ltd.
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A new compound called SR9011 increases metabolism, fat burning, and muscle growth in the lab.
Scientists at The Scripps Research Institute (TSRI) have successfully tested a drug, called SR9011,
in mice that kickstarts metabolism and results in increased muscle development.
Essentially, it's an exercise regime in a pill.
SR9011 alters the metabolic profile of skeletal muscle in a manner similar to the changes observed [in]
animals [that] are endurance trained. Basically, the drug sends a signal to the muscle to tell it to modify
its metabolism.
Half of the mice studied showed improved running endurance in terms of both time and distance. What was clearly interesting was that a small, drug-like molecule could increase metabolic rate in skeletal muscle and increase exercise endurance
There's no way to sugarcoat it-though many have tried-maintaining a healthy weight can be difficult. Because it's hard, many have tried "miracle" weight-loss pills and other quick fixes for something that ultimately requires a lifestyle change. Many over-the-counter diet and weigh-loss pills are unregulated
and may contain dangerous ingredients. SR9011, however, isn't like appetite suppressants, laxatives, or "fat blockers." And you won't find SR9011 in the ingredient lists of protein powders or exercise supplements.
The difference between SR9009 and other diet pills is in its chemistry. SR9011 is not an appetite
suppressant-as many weight-loss drugs are-and directly works by increasing the metabolic rate of muscle. Your metabolism speeds up and slows down naturally during the day, meaning that sometimes food is used for energy and sometimes it's stored as fat. By re-synching a dysfunctional metabolic clock, SR9011 ensures that food and excess fat are used as energy.
SR9011 is one of a pair of compounds developed at TSRI by Burris and his team. The drug binds to Rev-erbα,a natural protein in the body that influences lipid and glucose metabolism in the liver, inflammatory responses, and fat-storing cells. By binding to Rev-erbα, SR9011 can kickstart metabolism with another pleasant side-effect: increased muscle strength.
SR9011 is a trifunctional methacrylate monomer that provides exceptional adhesion to metal substrates. SR9011 is recommended for use in peroxide cured coatings, sealants, and PVC-based plastisols. Usage levels of 5% to 10% by weight are recommended.
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 diseases.
Compounds were synthesized by reductive amination of 5-nitro-2-thiophenecarboxaldehyde with 4-chlorobenzylamine and sodium triacetoxyborohydride yielded the secondary amine. A second reductive amination with 1-Boc-pyrrolidine-3-carboxaldehyde yielded the tertiary amine. This compound was treated with trifluoroacetic acid to remove the Boc-protecting group, and then reacted with either ethyl chloroformate (SR9009) or pentyl isocyanate (SR9011) to give the desired products.
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