(GLP-2 Tirz) – Technical Brief (For Research-Use-Only)
1. Identity
(GLP2) known in the pharmaceutical industry as Tirzepatide is a 39-amino-acid, lipid-modified peptide that binds and activates both the glucose-dependent insulinotropic polypeptide receptor (GIPR) and the glucagon-like peptide-1 receptor (GLP-1R) A. Albumin binding via its C20 di-acid side chain extends the circulation half-life to roughly one week, enabling once-weekly dosing in clinical settings B.
2. Mechanistic Highlights
1. β-cell stimulation (glucose-dependent) – Gs-coupled signalling increases intracellular cAMP and drives insulin granule exocytosis only when plasma glucose is elevated.
2. α-cell suppression – GLP-1R activation dampens glucagon release, curbing hepatic glucose output.
3. Delayed gastric emptying – Enteric–vagal feedback slows nutrient transit, blunting post-prandial glycaemic spikes.
4. Central appetite modulation – Engagement of GIPR/GLP-1R in hypothalamic nuclei reduces hunger, contributing to body-mass reduction seen in trials.
3. Safety Profile (clinical data)
GI:-
(Common) may cause Nausea, diarrhoea, transient vomiting.
(Severe/Rare) gastroparesis
Endocrine:-
(Common) N/A
(Severe/Rare) C-cell tumours in rodents → contraindication in MEN-2 / MTC
Pancreas:-
(Common) N/A)
(Severe/Rare) Low-frequency acute pancreatitis reports
CV:-
(Common) Mean heart-rate rise ~4–6 bpm (Severe/Rare) Cardiovascular outcome study ongoing
Overall, trials highlight robust glycaemic and weight improvements with a safety profile broadly similar to single-agent GLP-1 analogues
Important: these findings derive from regulated human studies. No safety data exist for unregulated human use.
4. Legal Position in the United Kingdom
• Tirzepatide is not scheduled under the Misuse of Drugs Act and is not a controlled substance.
• When supplied “FOR RESEARCH USE ONLY” (in-vitro, ex-vivo, or animal work), it sits outside the Human Medicines Regulations 2012.
• Any supply, advertisement, or discussion implying human therapeutic or weight-loss use reclassifies the product as a medicinal product, putting it under MHRA enforcement.
5. Practical Laboratory Handling
Reconstitution: use sterile 0.9 % Benzyl alcohol Bacteriostatic water, 1–3 mL⁻¹; swirl gently—avoid vigorous shaking.
• Storage: aliquot, −80 °C long term; ≤ 30 days at −20 °C once re-suspended.
• Typical exploratory dosing (rodent): 2.5–15mg subcutaneously, once weekly.
Bottom line:
Tirzepatide is a potent dual-incretin agonist with well-documented metabolic effects in regulated trials. Within the UK it may be purchased, possessed, and used solely as a laboratory research reagent; any use or promotion beyond that scope violates medicines legislation.
