Tirzep

• Dual Mechanism: Simultaneously targets both GIP and GLP-1 receptors for synergistic metabolic regulation 
• Imbalanced Activation: Greater occupancy of GIP receptor than GLP-1 receptor, creating a unique pharmacological profile 
• Biased Signaling: Favors cAMP generation over β-arrestin recruitment at the GLP-1 receptor, reducing internalization and enhancing insulin secretion 
• High Stability: Lyophilized formulation ensures long-term storage stability

Tirzepatide exerts its pharmacological effects through simultaneous activation of the GIP receptor (GIPR) and GLP-1 receptor (GLP-1R) :

1. Glycemic Control

• Glucose-dependent insulin secretion: Stimulates pancreatic β-cell insulin release under hyperglycemic conditions with low hypoglycemia risk 
• Glucagon suppression: Reduces hepatic glucose output 
• Improved β-cell function: Enhances insulin sensitivity and β-cell function 

2. Body Weight Regulation

• Central appetite suppression: Acts on hypothalamic appetite-regulating centers to increase satiety and reduce hunger signals 
• Delayed gastric emptying: Prolongs post-meal satiety
• Adipose tissue modulation: GIP component improves adipose tissue insulin sensitivity and reduces ectopic fat accumulation 

3. Unique Pharmacological Properties

Unlike native GLP-1, Tirzepatide exhibits biased agonism at the GLP-1 receptor – preferentially activating cAMP pathways over β-arrestin recruitment, resulting in less receptor desensitization and internalization, which may enhance efficacy . Additionally, it demonstrates imbalanced dual activation with higher affinity for GIPR than GLP-1R .

It is recommended to reconstitute using sterile saline or the specified buffer.

Use individually or in combination, as specified in the experimental design.

Store lyophilized powder sealed and protected from light at -20°C or below. After reconstitution, aliquot and freeze （-80°C）to avoid repeated freeze-thaw cycles to maintain peptide stability.

Specific dosage, frequency, and administration routes should be optimized based on published literature and preliminary experimental results, while strictly adhering to animal research ethical guidelines.

Packaging Note: This product is supplied in a sealed, sterile glass vial without any pre‑printed labels. This design supports institutional compliance protocols and allows researchers to apply custom labels that align with specific experimental protocols, ethical approvals, and local regulations. A separate document containing complete product details (name, batch number, purity, content, COA reference, etc.) is included for label customization and record‑keeping.