Tirzepatide

Tirzepatide selectively binds to and activates both the GIP and GLP-1 receptors, the targets for native GIP and GLP-1. Receptor pharmacology studies reveal that tirzepatide is an imbalanced and biased dual agonist: it engages the GIP receptor (GIPR) to a greater degree than the GLP-1 receptor (GLP-1R), and displays biased signaling at the GLP-1R to favor cAMP generation over β-arrestin recruitment, coincident with a weaker ability to drive GLP-1R internalization compared with GLP-1. This unique pharmacological profile enhances insulin secretion (first- and second-phase) and reduces glucagon levels, both in a glucose-dependent manner. GIP also plays a role in nutrient and energy metabolism, while GLP-1 delays gastric emptying, suppresses appetite, and improves satiety.

• Type 2 Diabetes Mellitus: Investigated as a therapeutic agent for glycemic control, demonstrating superior efficacy in lowering HbA1c compared with selective GLP-1 receptor agonists.
• Obesity and Weight Management: Employed in preclinical and clinical studies to evaluate significant and sustained weight reduction, with effects approaching those achieved with bariatric surgery.
• Cardiometabolic Diseases: Studied for beneficial effects on heart failure with preserved ejection fraction, metabolic dysfunction–associated steatohepatitis (MASH), and cardiovascular outcomes.
• Emerging Applications: Investigated for potential benefits in chronic kidney disease, neurological disorders including Alzheimer's and Parkinson's diseases, and alcohol use disorder.

CAS Number: 2023788-19-2
PubChem CID: 156588324
Molecular Formula: C₂₂₅H₃₄₈N₄₈O₆₈
Molecular Weight: 4,813.53 g/mol
Purity: ≥ 99% (batch-dependent; please refer to the Certificate of Analysis)
Form: White to off-white lyophilized powder
Storage: Store at ≤ -20°C in a cool, dry place, protected from light and moisture
Solubility: Soluble in water and DMSO; prepare working solutions per laboratory protocol