Dulaglutide is a glucagon-like peptide-1 receptor agonist (GLP-1 agonist) consisting of GLP-1(7-37) covalently linked to an Fc fragment of human IgG4. Dulaglutide binds to glucagon-like peptide 1 receptors, slowing gastric emptying and increases insulin secretion by pancreatic Beta cells. Simultaneously the compound reduces the elevated glucagon secretion by inhibiting alpha cells of the pancreas. GLP-1 is normally secreted by L cells of the gastrointestinal mucosa in response to a meal.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
|Solubility||Soluble in water|
Longer acting GLP-1 receptor agonists and the potential for improved cardiovascular outcomes: a review of current literature.
Tibble CA, et al. Expert Rev Endocrinol Metab. 2013 May;8(3):247-259. PMID: 30780817.
Regulation of glucose homeostasis by GLP-1.
Nadkarni P, et al. Prog Mol Biol Transl Sci. 2014;121:23-65. PMID: 24373234.
|Related Glucagon Receptor Products|
PF-06882961 is a potent, orally bioavailable agonist of the glucagon-like peptide-1 receptor (GLP-1R) agonist.
Teduglutide is a glucagon-like peptide-2 (GLP- 2) receptor agonist used for the treatment of short-bowel syndrome.
NNC0640 is a potent, negative allosteric modulator (NAM) of human G-protein-coupled glucagon receptor (GCGR) with IC50 of 69.2 nM.
|Avexitide (Exendin 9-39)
Avexitide (Exendin 9-39) is a specific and competitive GLP-1 receptor antagonist.
Cotadutide acetate is a potent peptide dual agonist of glucagon-like peptide-1 (GLP-1) and glucagon receptor, with EC50 values of 6.9 pM and 10.2 pM, respectively.
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