glucagon receptor

Glucagon receptor antagonists-5 is an orally bioavailable indazole-based glucagon receptor antagonist (Ki: 32 nM). It has potential for the treatment of type 2 diabetes mellitus (T2DM).

Semaglutide TFA is a glucagon-like peptide-1 congener that induces weight loss, lowers blood glucose levels, and reduces cardiovascular risk in diabetic patients.Semaglutide TFA induces mild-to-moderate and transient gastrointestinal disturbances, and may be used in the study of type 2 diabetes and obesity.

Semaglutide is a long-acting, selective, competitive GLP-1R agonist and a long-acting analog of human glucagon-like peptide-1, exhibiting potent hypoglycemic, weight-loss, cardioprotective, and neuroprotective effects. Upon activation of the GLP-1R, semaglutide promotes insulin secretion, inhibits gastric emptying and appetite, while also enhancing autophagy and suppressing oxidative stress and apoptosis. Semaglutide also plays a role in regulating mitochondrial function and lipid metabolism. Semaglutide is being investigated for use in type 2 diabetes, obesity, Parkinson’s disease, metabolic and fatty liver diseases (MASLD), and other neurodegenerative and liver diseases, as well as in cancer research.

Semaglutide Acetate is a GLP-1R agonist (EC50=6.2 pM) with long-acting, selective, competitive, and oral efficacy. Semaglutide acetate can be used in the study of type 2 diabetes.

Exendin-4 (Exenatide) is a glucagon-like peptide-1 receptor (GLP-1) agonist (IC₅₀: 3.22 nM). Exenatide is a 39 amino acid peptide. Compared to GLP-1, exenatide has a longer half-life of 2.4 hours.

LSN3318839 is a small-molecule compound and a positive allosteric modulator of the glucagon-like peptide-1 receptor (GLP-1R), featuring oral activity and selective enhancement of G protein-coupled signaling, which promotes glucose-dependent insulin secretion for blood glucose reduction.

Liraglutide (Liraglutida) is a synthetic analog of glucagon-like peptide-1 (GLP-1), an agonist of the GLP-1 receptor. Liraglutide can be used to treat type 2 diabetes and chronic obesity.

Tirzepatide (LY3298176) is a long-acting glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide-1 (GLP-1) receptor dual agonist. In HEK293 cells, it can effectively stimulate cAMP accumulation, with an EC50 of 0.0224 nM for the GIP receptor (GIPR) and an EC50 of 0.934 nM for the GLP-1 receptor (GLP-1R).

Tirzepatide (LY3298176) Acetate (2023788-19-2 free base) is a new molecule that can control blood glucose levels by combining dual agonism of glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide-1 (GLP-1) receptors.[3]

Tirzepatide sodium salt (LY3298176 sodium salt) is a GIP and GLP-1 receptor agonist with neuroprotective activity and can be used to treat obesity.

Avexitide (Exendin-3(9-39)amide) is a specific, competitive GLP-1 receptor antagonist (Ki = 0.36 nM). Avexitide binds to the GLP-1 receptor (GLP-1R) with high affinity (Kd = 0.42 nM), blocking the interaction between endogenous GLP-1 and the receptor, thereby counteracting the effects of excessive GLP-1 secretion. Avexitide is being studied for post-bariatric hypoglycemia (PBH) and congenital hyperinsulinism.

LGD-6972 is an antagonist of glucagon receptor.

(S,R)-LSN 3318839 enhances GLP-1R, shows strong blood sugar lowering in animals, works with sitagliptin.

6α-Methylprednisolone 21-hemisuccinate sodium salt (Asmacortone), a water-soluble ester, is used for allergic, cardiac, and hypoxic emergencies.

Oxyntomodulin acetate, a 37-amino acid peptide hormone, is a glucagon-like peptide 1 (GLP-1) receptor agonist[1].

V-0219 hydrochloride, an orally-active positive allosteric modulator (PAM) of the glucagon-like peptide-1 receptor (GLP-1R), is utilized in obesity-associated diabetes research.

1H-Benzimidazole-6-carboxylic acid is a GLP-1 receptor agonist.

Secretin (33-59), rat (Secretin (rat)) is a classical hormone in the gastrointestinal system and a neuropeptide.

PF-06882961 is an orally bioavailable glucagon-like peptide-1 receptor (GLP-1R) agonist.

Adomeglivant (LY2409021) is a potent and selective glucagon receptor antagonist. Which is used in clinical trial for type 2 diabetes mellitus.

GLP-1R Antagonist 1 is an orally active, CNS penetrant and non-competitive glucagon-like peptide 1 receptor (GLP-1R) antagonist (IC₅₀: 650 nM).

Glucagon (1-29), bovine, human, porcine is a hormone produced by pancreatic α-cells with glucagon activity, which promotes glycogenolysis and gluconeogenesis, and is used in the study of obesity and diabetes.

Glucagon (1-29), bovine, human, porcine hydrochloride (Porcine glucagon hydrochloride) is a peptide hormone produced by pancreatic α-cells that activates HNF4α, increases HNF4α phosphorylation, and stimulates gluconeogenesis.

3-Deoxyglucosone(3-Deoxy-D-glucosone) is synthesized by the intermediate pathway of the melad and polyol reactions.3-Deoxyglucosone reacts rapidly with protein amino groups to form advanced glycosylated end proteins (AGEs).3-Deoxyglucosone inactivates glutathione peroxidase and synergizes with low glucose to enhance GLP-1 secretion.3-Deoxyglucosone is used as a biomarker for diabetes mellitus.3-Deoxyglucosone has been shown to be an inhibitor of GLP-1 secretion in the presence of low glucose. 3-Deoxyglucosone inactivates glutathione oxidase, synergizes with low glucose to enhance GLP-1 secretion, and can be used as a biologic marker for diabetes.