Tirzepatide

同義語： Tirzepatide, LY3298176, GIP/GLP-1 receptor agonist, Dual incretin agonist, Mounjaro, Zepbound

Tirzepatide is a synthetic 39-amino acid peptide engineered as a dual agonist of the glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide-1 (GLP-1) receptors. Its backbone incorporates non-proteinogenic amino acids, including alpha-aminoisobutyric acid (Aib), and carries a C20 fatty diacid moiety attached via a linker to lysine at position 20. This structural design confers resistance to DPP-4 degradation and extends the plasma half-life to approximately five days, enabling once-weekly subcutaneous dosing.

Originally developed by Eli Lilly and Company under the code LY3298176, tirzepatide is produced through solid-phase peptide synthesis followed by high-performance liquid chromatography (HPLC) purification. It is supplied as a lyophilized powder for research and pharmaceutical compounding, with a purity typically ≥98%. The molecule is freely soluble in water and aqueous buffers at physiological pH, and its stability is maintained when stored desiccated at -20°C.

In the research setting, tirzepatide serves as a reference standard for studying incretin receptor co-activation, insulinotropic effects, and weight management pathways. Its unique dual mechanism has made it a focal point in metabolic disorder research, particularly for type 2 diabetes and obesity. For B2B buyers, tirzepatide is available in gram-scale quantities with full documentation to support formulation development and clinical trials.

化学構造と性質

The primary structure of tirzepatide is based on the native GIP sequence but includes key modifications: Aib substitutions at positions 2 and 13, a C-terminal amide, and a C20 diacid conjugated to the side chain of Lys20 via a γGlu-OEG-OEG linker. These modifications enhance metabolic stability and promote albumin binding, which slows renal clearance. The molecular formula is C225H348N48O68, and the monoisotopic mass is approximately 4813.45 Da. The lyophilized powder appears as a white to off-white cake, and its purity is routinely confirmed by reverse-phase HPLC and mass spectrometry.

作用機序

• GIP receptor agonism: Tirzepatide binds to and activates the GIP receptor, enhancing glucose-dependent insulin secretion and improving insulin sensitivity in peripheral tissues.
• GLP-1 receptor agonism: It also activates GLP-1 receptors, leading to increased satiety, delayed gastric emptying, and reduced glucagon release.
• Dual incretin effect: The simultaneous activation of both receptors produces complementary effects on glycemic control and energy balance, which are not observed with selective GLP-1 agonists.
• Albumin binding: The fatty diacid moiety facilitates high-affinity binding to serum albumin, extending the half-life and allowing for once-weekly administration.

品質仕様

供給および書類

• 容量: Monthly production capacity of 10 kg, scalable to 50 kg upon request.
• リードタイム: 3～5営業日（在庫品）
• ドキュメント: COA, MSDS, TDS, and HPLC/MS spectra provided with each shipment.
• パッケージ: 1 mg, 5 mg, 10 mg, 50 mg, or 100 mg in amber glass vials with rubber stoppers and aluminum seals; custom packaging available.

見積依頼

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