Dual GIP and GLP-1 receptor agonist with exceptional binding affinity. Studied for beta-cell function, insulin sensitivity modulation, delayed gastric emptying, and satiety signalling in preclinical metabolic disorder research models.
Tirzepatide is a novel dual-agonist peptide developed by Eli Lilly (trade names Mounjaro for T2D, Zepbound for obesity). It selectively engages both glucose-dependent insulinotropic polypeptide receptor (GIP-R) and glucagon-like peptide-1 receptor (GLP-1R) — the two principal incretin receptors. A C20 fatty diacid moiety enables albumin binding, extending half-life to ~5 days for sustained once-weekly dosing protocols in research.
Tirzepatide's amino-acid sequence is balanced for dual receptor affinity — favouring GIP-R activation while maintaining GLP-1R potency. This balanced agonism distinguishes it from single-receptor incretins.
The C20 lipid moiety enables non-covalent albumin binding, protecting Tirzepatide from rapid renal clearance and DPP-IV degradation. Half-life extends to ~5 days, enabling once-weekly research dosing.
Effects are mediated through pancreas (insulin release), gastrointestinal tract (gastric emptying), liver (hepatic glucose output), and CNS (appetite). Adipose tissue remodelling occurs secondary to caloric reduction and altered substrate utilisation.
The SURPASS Phase III trial series established Tirzepatide as approved therapy for Type 2 Diabetes. Mean HbA1c reductions of 2.0–2.5% and body-weight reductions of 8–15% across dose tiers (5/10/15 mg weekly) inform broader research into dual-incretin mechanisms.
Refs: Frías JP et al., N Engl J Med (2021); Rosenstock J et al., Lancet (2021)
SURMOUNT-1 demonstrated mean body-weight reduction of 22.5% at the 15mg dose over 72 weeks — the largest observed for any peptide therapeutic. This established Tirzepatide's effectiveness profile and motivated extensive preclinical mechanism research.
Refs: Jastreboff AM et al., N Engl J Med (2022)
Each batch is independently tested by a third-party ISO-accredited laboratory. The analysis below reflects Batch AV-2025-TIR-038, tested 05 March 2025.
| Test Parameter | Method | Specification | Result | Status |
|---|---|---|---|---|
| Identity | ESI-MS / MS-MS | Matches theoretical m/z | Confirmed (4814 Da) | PASS |
| Purity (HPLC) | RP-HPLC C18, 210nm | ≥98.0% | 99.5% | PASS |
| Water content | Karl Fischer | ≤8.0% | 4.9% | PASS |
| Heavy metals | ICP-MS | ≤10 ppm | <2 ppm | PASS |
| Endotoxins | LAL chromogenic | ≤10 EU/mg | <1 EU/mg | PASS |
| Form | Temperature | Duration |
|---|---|---|
| Lyophilised powder | −20°C (preferred) or 2–8°C | 24 months / 12 months |
| Reconstituted (BAC water) | 2–8°C | ≤28 days |
Wipe vial with 70% IPA.
For 5 mg vial, add 2 mL BAC water → 2.5 mg/mL stock. Inject slowly along the inner wall.
Swirl gently. Dissolution typically completes within 60 seconds.
2–8°C, light-protected. Aliquot for repeated weekly use to minimise vial-membrane penetration.
Semaglutide is a selective GLP-1 receptor agonist. Tirzepatide engages both GLP-1 AND GIP receptors. The additional GIP receptor activity contributes to greater body-weight reduction (~22% vs ~15% for semaglutide at top doses) and may improve insulin sensitivity beyond GLP-1 alone. Head-to-head trials (SURPASS-2) directly compared the two at similar dose tiers.
GIP and GLP-1 receptors mediate complementary effects: GLP-1 dominates in central appetite control and gastric emptying; GIP plays a larger role in insulin sensitivity, beta-cell function, and adipose-tissue lipid handling. Engaging both produces effects that exceed the sum of their individual contributions in published research models.
The C20 fatty diacid modification enables albumin binding, extending half-life to ~5 days. This pharmacokinetic profile allows once-weekly dosing in research protocols while maintaining therapeutic plasma concentrations throughout the dosing interval. Daily dosing is not required and would not improve outcomes.
Standard preclinical and clinical research follows escalating titration: 2.5mg weekly for 4 weeks, then 5mg, 7.5mg, 10mg, 12.5mg, 15mg with 4-week intervals. This gradual escalation minimises gastrointestinal adverse effects characteristic of incretin agonists. Maximum tolerated dose varies across research models.
Independently verified by third-party ISO-accredited laboratory. COA available on request.
View Tirzepatide in Store → Reconstitution Protocol Guide