Tirzepatide (sodium salt)

Tirzepatide is an agonist of glucagon-like peptide 1 receptor (GLP-1R) and gastric inhibitory polypeptide (GIP) receptor.1 It induces cAMP production in HEK293 cells expressing human GLP-1R or human GIP receptor (EC50s = 6.54 and 1.01 nM, respectively). Tirzepatide (100 nM) induces receptor internalization in HEK293 cells expressing human GLP-1R or GIP receptor. 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.2 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.3 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, weight management, and moderate-to-severe sleep apnea in adults with obesity.WARNING This product is not for human or veterinary use.

A dual GLP-1R and GIP receptor agonist

4813.5

≥95%

Biochemicals/Peptides/Receptor Pharmacology/Agonists

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;Synonyms:LY3298176

OC[C@@H](C(N)=O)NC([C@H]1N(C([C@H]2N(C([C@H]3N(C([C@H](C)NC(CNC([C@H](CO)NC([C@H](CO)NC([C@H]4N(C(CN

C225H348N48O68 • XNa

≥ 4 years

DMSO: Sparingly soluble: 1-10 mg/ml PBS (pH 7.2): Sparingly soluble: 1-10 mg/ml Water: Soluble: =10 mg/ml