Obesity|Inhibitors Agonists Modulators Antagonists|HmoBio.com

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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.

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
H9295	Danuglipron tromethamine	2230198-03-3	Danuglipron tromethamine is a potent, orally bioavailable agonist of the glucagon-like peptide-1 receptor agonist (GLP-1R).
H9213	PF-06882961	2230198-02-2	PF-06882961 is a potent, orally bioavailable agonist of the glucagon-like peptide-1 receptor.
H9014	MK-0557	328232-95-7	MK-0557 is a highly selective, orally available neuropeptide Y5 receptor antagonist with a Ki of 1.6 nM.
H8806	Cagrilintide	1415456-99-3	Cagrilintide is a potent Amylin receptor agonists.
H8767	Paltusotine	2172870-89-0	Paltusotine (CRN 00808) is an oral non-peptide somatostatin receptor 2 agonist, for the treatment of acromegaly.
H5073	JTT-553 benzosulfonate	701232-94-2	JTT-553 is a novel potent, selective DGAT-1 inhibitor with IC50 of 2.38 nM, shows no inhibitory activity for human DGAT2 and ACA T1 (IC50>10 uM); suppresses plasma TG and chylomicron TG levels after olive oil loading in Sprague-Dawley (SD) rats; also reduces daily food intake and body weight gain in diet-induced obesity rats.
H5072	JTT-553	701232-94-2	JTT-553 is a novel potent, selective DGAT-1 inhibitor with IC50 of 2.38 nM, shows no inhibitory activity for human DGAT2 and ACA T1 (IC50>10 uM); suppresses plasma TG and chylomicron TG levels after olive oil loading in Sprague-Dawley (SD) rats; also reduces daily food intake and body weight gain in diet-induced obesity rats.
H5069	DGAT1-IN-4	942999-61-3	A potent, selective, and orally efficacious inhibitor of DGAT-1 with IC50 of 15 nM and 9 nM for hDGAT-1 and mDGAT-1, respectively; shows no significant activity for ACAT-1 (IC50=5.2 uM); shows effectivity in both intestinal and adipose tissue, reduces body weight or body weight gain following oral administration in both mouse and rat models of dietary-induced obesity.
H4987	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.
H4971	Beloranib hemioxalate	529511-79-3	An analog of the natural compound Fumagillin that functions as a highly potent methionine aminopeptidase 2 (MetAP2) inhibitor; strongly inhibit the growth of cancers in xenografted nude model; also causes significant body weight and appetite reduction an anti-obesity agent.

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