Tirzepatide-RUO 10mg

Tirzepatide (also known as LY3298176) is a synthetic, long-acting dual agonist peptide that activates both the glucose-dependent insulinotropic polypeptide receptor (GIPR) and the glucagon-like peptide-1 receptor (GLP-1R). This 39-amino-acid linear peptide is engineered from a GIP backbone with multiple modifications for enhanced stability, receptor affinity, and pharmacokinetics. Key structural features include:
• Substitution with α-aminoisobutyric acid (Aib) at positions 2 and 13 to confer resistance to dipeptidyl peptidase-4 (DPP-4) degradation and improve helix stability.
• Acylation at the lysine residue at position 20 (Lys²⁰) with a C20 fatty diacid (eicosanedioic acid) linked via a hydrophilic spacer consisting of γ-glutamic acid (γ-Glu) and two units of 8-amino-3,6-dioxaoctanoic acid (OEG or AEEA), enabling reversible binding to serum albumin for prolonged circulation.
• C-terminal amidation (serinamide) for additional stability and receptor interaction optimization. The approximate molecular formula is C₂₂₅H₃₄₈N₄₈O₆₈, with a molecular weight of ~4810–4813 Da. A representative sequence incorporating modifications is: Y-(Aib)-EGTFTSDYSI-(Aib)-LDK-[acylated Lys]-IAQKAFVQWLIAGGPSSGAPPPS-NH₂ (where acylated Lys includes the γ-Glu-2×OEG-C20 diacid moiety).
Supplied as high-purity lyophilized powder (>98% purity, verified by HPLC and mass spectrometry), Tirzepatide is intended exclusively for in vitro research and scientific experimentation. It is commonly utilized in preclinical laboratory models to investigate dual incretin receptor agonism mechanisms, synergistic effects on insulin secretion, glucagon suppression, glucose homeostasis, appetite regulation, gastric emptying dynamics, energy balance, lipid metabolism, and related signaling pathways (e.g., cAMP production, β-arrestin recruitment) in cellular assays, tissue models, or animal systems exploring metabolic regulation, type 2 diabetes models, obesity, and neuroendocrine processes.