Tirzepatide¶
Tirzepatide (CAS 2023788-19-2) is a first-in-class dual glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide-1 (GLP-1) receptor agonist with a molecular weight of approximately 4,813 Da. This 39-amino acid synthetic peptide incorporates a C20 fatty diacid moiety conjugated via a AEEA-γ-Glu linker, conferring albumin binding and an extended pharmacokinetic profile. By simultaneously engaging both incretin receptors, tirzepatide achieves amplified glycemic control and weight-modulatory effects compared to selective GLP-1 receptor activation.
Technical Specifications¶
| Property | Value |
|---|---|
| CAS Number | 2023788-19-2 |
| Molecular Formula | C₂₂₅H₃₄₈N₄₈O₆₈ |
| Molecular Weight | ~4,813 Da |
| Purity | ≥99% (HPLC-verified) |
| Appearance | Lyophilized white powder |
| Solubility | Soluble in phosphate-buffered saline (pH 7.4); limited aqueous solubility |
| Storage | -20°C (lyophilized), 2–8°C (reconstituted) |
Mechanism of Action¶
Tirzepatide functions as a balanced dual agonist at the GIP receptor (GIPR) and GLP-1 receptor (GLP-1R), both class B GPCRs coupled to Gαs/cAMP signal transduction. At the GLP-1R, it stimulates glucose-dependent insulin secretion from pancreatic β-cells, inhibits glucagon release from α-cells, and delays gastric emptying. At the GIPR, it enhances cAMP-mediated insulinotropic signaling while also promoting lipid buffering in white adipose tissue through enhanced lipoprotein lipase activity and reduced lipolysis. The biased signaling profile of tirzepatide at GIPR — favoring cAMP over β-arrestin recruitment — is proposed to contribute to its superior metabolic efficacy. The C20 fatty diacid chain enables reversible binding to serum albumin, extending the half-life to approximately 5 days and enabling once-weekly research protocols.
Research Applications¶
- Primary: Type 2 diabetes research — dual incretin receptor pharmacology, glycemic regulation, insulin sensitivity
- Secondary: Obesity intervention models, metabolic syndrome studies, non-alcoholic fatty liver disease (NAFLD) research
- Model Systems: In vitro (INS-1 832/13 cells, human islet preparations), in vivo (diet-induced obese murine models, Zucker diabetic fatty rats)
Quality Control & Analytical Methods¶
- HPLC: ≥99% purity verification at 214/220 nm (C18 reversed-phase column)
- Mass Spectrometry: ESI-MS for molecular weight confirmation (~4,813 Da)
- Peptide Content: Amino acid analysis (AAA) for net peptide content determination
- Endotoxin: <1 EU/mg (LAL assay)
- TFA Content: <1% (ion chromatography)
Stability & Storage¶
| Condition | Stability |
|---|---|
| -20°C (lyophilized) | 24 months |
| 4°C (lyophilized) | 6 months |
| 25°C (lyophilized) | 1 month |
| Reconstituted (4°C) | 7 days |
| Reconstituted (-20°C) | 30 days |
Key Research References¶
- Coskun et al. (2018) — LY3298176, a novel dual GIP and GLP-1 receptor agonist for the treatment of type 2 diabetes mellitus. Mol Metab. PMID: 30473097
- Frias et al. (2018) — Efficacy and safety of LY3298176, a novel dual GIP and GLP-1 receptor agonist, in patients with type 2 diabetes (SURPASS-1). Lancet. PMID: 30293770
- Jastreboff et al. (2022) — Tirzepatide once weekly for the treatment of obesity (SURMOUNT-1). N Engl J Med. PMID: 35658024
Source & Purchase¶
For researchers requiring research-grade TIRZEPATIDE with full analytical documentation including HPLC, LC-MS, and Certificate of Analysis, visit the HK Peptides product page for specifications, bulk pricing, and ordering.
Related Molecules¶
- Semaglutide — Selective GLP-1 receptor agonist
- Retatrutide — Triple GIP/GLP-1/GCG receptor agonist
- Cagrilintide — Long-acting amylin analog
- All Product Specifications
FAQ¶
Q: What purity level is standard for Tirzepatide? A: HK Peptides supplies Tirzepatide at ≥99% purity by HPLC with full COA documentation.
Q: How should Tirzepatide be stored for research use? A: Lyophilized Tirzepatide should be stored at -20°C. Reconstituted solutions at 4°C for short-term use (up to 7 days); aliquot and freeze at -20°C for extended storage.