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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's disease. See also * GSK4112 * SR9009 * 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 {{pharm-stub Isoquinolines ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 density, and inflammation. See also * SR8278 * SR9009 * 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 {{pharm-stub Thiophenes Tert-butyl compounds Nitro compounds Chlorobenzene derivatives Amines Esters ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
SR9009
SR9009, also known as Stenabolic, is a research drug that was developed by professor Thomas Burris of the Scripps Research Institute as an agonist of Rev-ErbA (i.e., increases the constitutive repressor, repression of Regulation of gene expression, genes regulated by Rev-ErbA) with a half-maximum inhibitory concentration (IC50, IC50) = 670 nM for Rev-ErbA alpha, Rev-ErbAα and IC50 = 800 nM for Rev-ErbA beta, Rev-ErbAβ. Activation of Rev-ErbA-α by SR9009 in mice increases exercise capacity by increasing mitochondria counts in skeletal muscle. Abuse of SR9009 has been reported within the bodybuilding community, resulting in SR9009 being placed on the World Anti-Doping Agency list of List of drugs banned by WADA, prohibited drugs. SR9009 and the related SR9011 drug are described as "Hormone and Metabolic Modulators". See also * GSK4112 * GW501516 * SR8278 * SR9011 References Amines Benzene derivatives Experimental drugs Thiophenes {{pharma-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 IC50 = 560 nM for Rev-ErbA beta, Rev-ErbAβ. It has been used in the study of the regulation of the circadian rhythm and its links to immune system function, inflammation and cancer. See also * GSK-4112 * GW501516 * Nidufexor * SR8278 * SR9009 References Amines Benzene derivatives Experimental drugs Thiophenes Pentyl compounds {{pharma-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Rev-ErbA Alpha
Rev-Erb alpha (Rev-Erbɑ), also known as nuclear receptor subfamily 1 group D member 1 (NR1D1), is one of two Rev-Erb proteins in the nuclear receptor (NR) family of intracellular transcription factors. In humans, REV-ERBɑ is encoded by the ''NR1D1'' gene, which is highly conserved across animal species. Rev-Erbɑ plays an important role in regulation of the core circadian clock through repression of the positive clock element Bmal1. It also regulates several physiological processes under circadian control, including metabolic and immune pathways. Rev-Erbɑ mRNA demonstrates circadian oscillation in its expression, and it is highly expressed in mammals in the brain and metabolic tissues such as skeletal muscle, adipose tissue, and liver. Discovery Rev-Erbɑ was discovered in 1989 by Nobuyuki Miyajima and colleagues, who identified two ''erbA'' homologs on human chromosome 17 that were transcribed from opposite DNA strands in the same locus. One of the genes encoded a prot ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Duchenne Muscular Dystrophy
Duchenne muscular dystrophy (DMD) is a severe type of muscular dystrophy that primarily affects boys. Muscle weakness usually begins around the age of four, and worsens quickly. Muscle loss typically occurs first in the thighs and pelvis followed by the arms. This can result in trouble standing up. Most are unable to walk by the age of 12. Affected muscles may look larger due to increased fat content. Scoliosis is also common. Some may have intellectual disability. Females with a single copy of the defective gene may show mild symptoms. The disorder is X-linked recessive. About two thirds of cases are inherited from a person's mother, while one third of cases are due to a new mutation. It is caused by a mutation in the gene for the protein dystrophin. Dystrophin is important to maintain the muscle fiber's cell membrane. Genetic testing can often make the diagnosis at birth. Those affected also have a high level of creatine kinase in their blood. Although there is no know ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Alzheimer's Disease
Alzheimer's disease (AD) is a neurodegeneration, neurodegenerative disease that usually starts slowly and progressively worsens. It is the cause of 60–70% of cases of dementia. The most common early symptom is difficulty in short-term memory, remembering recent events. As the disease advances, symptoms can include primary progressive aphasia, problems with language, Orientation (mental), disorientation (including easily getting lost), mood swings, loss of motivation, self-neglect, and challenging behaviour, behavioral issues. As a person's condition declines, they often withdraw from family and society. Gradually, bodily functions are lost, ultimately leading to death. Although the speed of progression can vary, the typical life expectancy following diagnosis is three to nine years. The cause of Alzheimer's disease is poorly understood. There are many environmental and genetic risk factors associated with its development. The strongest genetic risk factor is from an alle ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
