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You are here:Home-Research Areas-Metabolic Disorder-Obesity

Request The Product List ofObesity Obesity

   Obesity is a metabolic condition that is characterized by an excess of body fat to the extent that it has a detrimental effect on health. Humans are classified as obese when their body mass index (BMI, weight in kilograms / (height in meters)2) is greater than 30. Obesity increases the risk of many other diseases, including cardiovascular disease, diabetes, sleep apnoea, osteoarthritis and some cancers. It is a major cause of morbidity and mortality and prevalence of this condition is increasing.

肥胖引起炎症。 内脏肥胖的脂肪组织通过MCP-1巨噬细胞浸润和促炎因子的分泌诱导慢性低度炎症。 但是,肥胖可能导致多种疾病的高发。

   Causes of Obesity

   The most common cause of obesity is a combination of low energy expenditure and high caloric intake. Environmental factors play a role in some cases and numerous susceptibility genes have been identified, including agouti-related peptide (AgRP) 199G - A polymorphism, FTO, NPC1, leptin, leptin receptors (Ob-R), and prohormone convertase-1. Certain psychiatric illnesses are associated with obesity, as are some genetic syndromes including Prader-Wili syndrome and MOMO syndrome. In addition, obesity can be secondary to other conditions such as hypothyroidism, Cushing's syndrome and growth hormone deficiency.

    Many endogenous peptides effect appetite and hence have an influence on energy intake. Peripheral hormones effecting appetite include ghrelin, adiponectin, leptin, insulin, peptide YY (3-36), pancreatic polypeptide, glucagon-like peptide 1 (GLP-1), oxyntomodulin, amylin, cholecystokinin and bombesin. Other peptides act centrally to control appetite and these include neuropeptide Y, AgRP, melanocortin, orexin, galanin, α-melanocyte-stimulating hormone (α-MSH), cocaine and amphetamine-related transcript (CART) and neurotensin (NT).

   Therapeutics

   Treatment for obesity is focused on decreasing caloric intake and increasing energy expenditure. However, pharmacological interventions are available and include: orlistat, which inhibits pancreatic lipase to prevent uptake of fat from the diet; sibutramine, a serotonin-noradrenalin reuptake inhibitor (SNRI) that acts as an appetite suppressant; and rimonabant, a cannabinoid CB1 receptor inverse agonist. These drugs only have a modest effect on weight. Other drugs, such as bupropion, are used 'off label' for their appetite-suppressing effects.

    Due to the prevalence and economic burden produced by obesity, novel pharmacological treatments are needed. Many are focusing on inhibiting the effects of orexigenic peptides and agonizing the effects of anorexigenic peptides to reduce appetite and subsequently reduce food intake. Current interest is focused on ghrelin receptor antagonists, peptide YY (3-36), GLP-1 analogs, amylin analogs and orexin 1 receptor (OX1) antagonists.

Cat. No. Product Name CAS No. Information
GY10388

MLN-4760

305335-31-3

MLN-4760 (MLN4760) is a potent, selective inhibitor of angiotensin-converting enzyme (ACE)-related carboxypeptidase ACE2 with IC50 of 0.44 nM (hACE2); displays >5,000-fold selectivity over related enzymes including human testicular ACE (IC50>100 uM) and bovine carboxypeptidase A (IC50=27 uM); exacerbated the Ang II-dependent formation of ROS and abolished the generation of Ang-(1-7) from Ang II; exacerbates cardiac hypertrophy and fibrosis in Ren-2 hypertensive rats.

GY10531

RO 27-3225

RO 27-3225 (RO27-3225, RO 273225) is a potent, selective melanocortin melanocortin receptor MC4R agonist with EC50 of 1 nM, >30-fold selectivity over MC3R; shows some activity at the MC1 receptor (EC50=8 nM), reverses hemorrhagic shock, reduces multiple organ damage, and improves survival.

GY04077

CP-945598

686347-12-6

A potent, and selective CB1 receptor antagonist with Ki of 0.7 nM/0.12 nM in binding and functional assays respectively; has low affinity (Ki=7600 nM) for human CB2 receptors; reverses cannabinoid agonist mediated responses, reduces food intake, and increases energy expenditure and fat oxidation in rodents.

GY04041

CP945598

686344-29-6

A potent, and selective CB1 receptor antagonist with Ki of 0.7 nM/0.12 nM in binding and functional assays respectively; has low affinity (Ki=7600 nM) for human CB2 receptors; reverses cannabinoid agonist mediated responses, reduces food intake, and increases energy expenditure and fat oxidation in rodents.

GY05695

CE-326597

870615-40-0

CE-326597 (CE 326597) is a potent, selective agonist of the human and rat CCK1 receptor with Ki of 36 nM; significantly reduces food intake with minimal systemic exposure in rodents.

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