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Nidufexor
Nidufexor (LMB-763) is a drug which acts as a partial agonist of the farnesoid X receptor (FXR). It has reached Phase II clinical trials for the treatment of diabetic nephropathy and nonalcoholic steatohepatitis. See also * GSK-4112 * 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 Farnesoid X receptor agonists {{pharm-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] |
Partial Agonist
In pharmacology, partial agonists are drugs that bind to and activate a given receptor, but have only partial efficacy at the receptor relative to a full agonist. They may also be considered ligands which display both agonistic and antagonistic effects—when both a full agonist and partial agonist are present, the partial agonist actually acts as a competitive antagonist , competing with the full agonist for receptor occupancy and producing a net decrease in the receptor activation observed with the full agonist alone. Clinically, partial agonists can be used to activate receptors to give a desired submaximal response when inadequate amounts of the endogenous ligand are present, or they can reduce the overstimulation of receptors when excess amounts of the endogenous ligand are present. Some currently common drugs that have been classed as partial agonists at particular receptors include buspirone, aripiprazole, buprenorphine, nalmefene and norclozapine. Examples of ligands acti ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Farnesoid X Receptor
The bile acid receptor (BAR), also known as farnesoid X receptor (FXR) or NR1H4 (nuclear receptor subfamily 1, group H, member 4), is a nuclear receptor that is encoded by the ''NR1H4'' gene in humans. Function FXR is expressed at high levels in the liver and intestine. Chenodeoxycholic acid and other bile acids are natural ligands for FXR. Similar to other nuclear receptors, when activated, FXR translocates to the cell nucleus, forms a dimer (in this case a heterodimer with RXR) and binds to hormone response elements on DNA, which up- or down-regulates the expression of certain genes. One of the primary functions of FXR activation is the suppression of cholesterol 7 alpha-hydroxylase (CYP7A1), the rate-limiting enzyme in bile acid synthesis from cholesterol. FXR does not directly bind to the CYP7A1 promoter. Rather, FXR induces expression of small heterodimer partner (SHP), which then functions to inhibit transcription of the CYP7A1 gene. In this way, a negative feedback ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Clinical Trial
Clinical trials are prospective biomedical or behavioral research studies on human participants designed to answer specific questions about biomedical or behavioral interventions, including new treatments (such as novel vaccines, drugs, dietary choices, dietary supplements, and medical devices) and known interventions that warrant further study and comparison. Clinical trials generate data on dosage, safety and efficacy. They are conducted only after they have received health authority/ethics committee approval in the country where approval of the therapy is sought. These authorities are responsible for vetting the risk/benefit ratio of the trial—their approval does not mean the therapy is 'safe' or effective, only that the trial may be conducted. Depending on product type and development stage, investigators initially enroll volunteers or patients into small pilot studies, and subsequently conduct progressively larger scale comparative studies. Clinical trials can vary i ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Diabetic Nephropathy
Diabetic nephropathy, also known as diabetic kidney disease, is the chronic loss of kidney function occurring in those with diabetes mellitus. Diabetic nephropathy is the leading causes of chronic kidney disease (CKD) and end-stage renal disease (ESRD) globally. The triad of protein leaking into the urine (proteinuria or albuminuria), rising blood pressure with hypertension and then falling renal function is common to many forms of CKD. Protein loss in the urine due to damage of the glomeruli may become massive, and cause a low serum albumin with resulting generalized body swelling (edema) so called nephrotic syndrome. Likewise, the estimated glomerular filtration rate (eGFR) may progressively fall from a normal of over 90 ml/min/1.73m2 to less than 15, at which point the patient is said to have end-stage renal disease. It usually is slowly progressive over years. Pathophysiologic abnormalities in diabetic nephropathy usually begin with long-standing poorly controlled blood g ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Nonalcoholic Steatohepatitis
Non-alcoholic fatty liver disease (NAFLD), also known as metabolic (dysfunction) associated fatty liver disease (MAFLD), is excessive fat build-up in the liver without another clear cause such as alcohol use. There are two types; non-alcoholic fatty liver (NAFL) and non-alcoholic steatohepatitis (NASH), with the latter also including liver inflammation. Non-alcoholic fatty liver is less dangerous than NASH and usually does not progress to NASH. When NAFL does progress to NASH, it may eventually lead to complications such as cirrhosis, liver cancer, liver failure, or cardiovascular disease. Obesity and type 2 diabetes are strong risk factors for NAFLD. Other risks include being overweight, metabolic syndrome (defined as at least three of the five following medical conditions: abdominal obesity, high blood pressure, high blood sugar, high serum triglycerides, and low serum HDL cholesterol), a diet high in fructose, and older age. NAFLD and alcoholic liver disease are typ ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
GSK-4112
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] |
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