Tirzepatide

Product Overview

Tirzepatide (development code LY3298176, brand names Mounjaro / Zepbound) is a 39-amino-acid synthetic peptide engineered on the native GIP sequence: the unnatural amino acid α-aminoisobutyric acid (Aib) is introduced at positions 2 and 13 to resist DPP-4 degradation; the C-terminus is amidated; and the Lys20 side chain is conjugated via a γ-glutamic acid and two AEEA (8-amino-3,6-dioxaoctanoic acid) spacers to 1,20-eicosanedioic acid (C20 fatty diacid). The fatty chain binds reversibly to plasma albumin (approx. 99%), extending the half-life to about 5 days and enabling once-weekly subcutaneous dosing. As a GIP / GLP-1 dual receptor agonist, it promotes first- and second-phase insulin secretion and suppresses glucagon in a glucose-dependent manner, outperforming selective GLP-1 receptor agonists in glycemic control and weight reduction.

Technical Specifications

• Standards: CHP / USP / EP
• Specification: 0.99 (purity ≥99.0%, HPLC); dosage form: injection
• CAS No.: 2023788-19-2
• Molecular formula: C₂₂₅H₃₄₈N₄₈O₆₈
• Molecular weight: 4813.45 g/mol (average mass, IUPAC 2007); monoisotopic mass 4810.52 Da
• Appearance: White to off-white lyophilized powder
• Purity (HPLC): ≥ 99.0%
• Melting point: No defined melting point — peptides generally denature and decompose stepwise on heating rather than melting; some commercial sources cite approximately 152–156 °C, for reference only and not a quality control specification
• Amino acid sequence: Tyr-Aib-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Tyr-Ser-Ile-Aib-Leu-Asp-Lys-Ile-Ala-Gln-Lys(C20 diacid-γGlu-(AEEA)₂)-Ala-Phe-Val-Gln-Trp-Leu-Ile-Ala-Gly-Gly-Pro-Ser-Ser-Gly-Ala-Pro-Pro-Pro-Ser-NH₂
• Solubility: Freely soluble in DMSO (≥50 mg/mL); soluble in water (pH ≈4.5), dilute acetic acid and phosphate buffer (pH 7.5, approx. 5 mg/mL), with sonication if necessary; insoluble / sparingly soluble in acetonitrile
• Specific rotation: −19.0° to −39.0° (calculated on the anhydrous, ion-free basis)
• Loss on drying (moisture): ≤ 10.0% (typical batches 1.2%–7.0%)
• Related substances: Any individual unknown impurity ≤0.5%; total impurities ≤2.0%
• Storage: Freeze at −20 °C, dry, protected from light and sealed (long-term); short-term storage at 2–8 °C is acceptable; reconstituted solutions should be stored at 2–8 °C and used within the specified period, avoiding repeated freeze–thaw cycles

Applications

• Type 2 diabetes (T2DM): As an adjunct to diet and exercise for the treatment of adults with inadequately controlled type 2 diabetes, administered by subcutaneous injection once weekly (Mounjaro, FDA approved May 13, 2022)
• Long-term weight management (obesity / overweight): For adults with obesity with BMI ≥28 kg/m², or overweight adults with BMI ≥24 kg/m² and at least one weight-related comorbidity (hypertension, dyslipidemia, hyperglycemia, obstructive sleep apnea, cardiovascular disease, etc.) (Zepbound)
• Obstructive sleep apnea (OSA): For moderate-to-severe OSA in adults with obesity; the FDA approved Zepbound for this indication in December 2024
• Investigational expansion directions: Clinical research in cardiovascular risk reduction, metabolic dysfunction-associated steatohepatitis (MASH) and other metabolic diseases
• CMO contract manufacturing: Compatible with injections, prefilled pens, multi-dose vials and lyophilized powder for reconstitution; as a peptide API for GMP-scale synthesis and CMO / CDMO contract manufacturing

Note: This product is an active pharmaceutical ingredient (API) intended solely for compliant industrial, research and pharmaceutical manufacturing use; it is not for end clinical use or guidance for self-administration.

Product information: please contact us. This information is for reference only.