Formulation: A solid
Formal Name: L-tyrosyl-2-methylalanyl-L-α-glutamylglycyl-L-threonyl-L-phenylalanyl-L-threonyl-L-seryl-L-α-aspartyl-L-tyrosyl-L-seryl-L-isoleucyl-2-methylalanyl-L-leucyl-L-α-aspartyl-L-lysyl-L-isoleucyl-L-alanyl-L-glutaminyl-N6-[(22S)-22,42-dicarboxy-1,10,19,24-tetraoxo-3,6,12,15-tetraoxa-9,18,23-triazadotetracont-1-yl]-L-lysyl-L-alanyl-L-phenylalanyl-L-valyl-L-glutaminyl-L-tryptophyl-L-leucyl-L-isoleucyl-L-alanylglycylglycyl-L-prolyl-L-seryl-L-serylglycyl-L-alanyl-L-prolyl-L-prolyl-L-prolyl-L-serinamide, sodium salt
Purity: ≥95%
Formula Markup: C225H348N48O68 • XNa
Formula Weight: 4813,5
Shelf life (days): 1460
Notes: Tirzepatide is an agonist of glucagon-like peptide 1 receptor (GLP-1R) and G protein-coupled receptor 119 (GPR119).{67582} It induces cAMP production in HEK293 cells expressing human GLP-1R or human GPR119 (EC50s = 6.54 and 1.01 nM, respectively). Tirzepatide (100 nM) induces receptor internalization in HEK293 cells expressing human GLP-1R or GPR119. In vivo, tirzepatide (10 nmol/kg per day) decreases body weight, food intake, plasma levels of leptin, triglycerides, and free fatty acids (FFAs), hepatic levels of triglycerides, and blood glucose levels in a mouse model of high-fat diet-induced obesity.{67583} It prevents A. alternata-induced increases in the numbers of eosinophils and lymphocytes in the bronchoalveolar lavage fluid (BALF) from A. alternata-challenged mice when administered at a dose of 50 nmol/kg every three days.{67584} Tirzepatide (50 nmol/kg every three days) inhibits bronchoconstriction induced by the muscarinic receptor agonist methacholine (acetyl-β-methylcholine; Item No. 23092) in a mouse model of diabetes-induced asthma. Formulations containing tirzepatide have been used in the treatment of type 2 diabetes mellitus.
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