Tirzepatide

Tirzepatide

Price range: $50.00 through $130.00

GLP-1 / GIP Dual Receptor Agonist · 39-Amino-Acid Lipidated Peptide

Tirzepatide (LY3298176) is a synthetic 39-amino-acid peptide derivative engineered to concurrently activate both glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide-1 (GLP-1) receptors. Built upon an endogenous GIP sequence backbone, it incorporates non-canonical α-aminoisobutyric acid (Aib) residues alongside a C₂₀ fatty-diacid side chain attached to Lys²⁰ via a γGlu-γGlu linker. This acylation enables strong, reversible albumin binding, yielding an in vivo elimination half-life of approximately 5 days. Extensive literature from the SURPASS and SURMOUNT trial series (Frías et al., 2021; Jastreboff et al., 2022) details its dual-incretin receptor pharmacology, imbalanced agonism profiles, biased intracellular cAMP signaling, and combined impacts on glycemic dynamics and central anorectic pathways.

Supplied at 5mg.

SKU: TIRZEP-PARENT Categories: ,

Description

Overview

Tirzepatide is a synthetic 39-amino-acid linear peptide engineered to co-activate both glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide-1 (GLP-1) receptors. Based on the endogenous GIP backbone sequence, it incorporates non-canonical α-aminoisobutyric acid (Aib) substitutions alongside a lipidated side chain.

A C₂₀ fatty-diacid conjugated to Lys²⁰ via a γGlu-γGlu di-peptide linker promotes strong, reversible binding to circulating serum albumin, yielding an in vivo elimination half-life of approximately 5 days.

Key Technical Specifications

Sequence YXEGTFTSDYSIXLDKIAQKAFVQWLIAGGPSSGAPPPS-NH2
(X = Aib; Lys20 conjugated to γGlu-γGlu-C20 diacid; C-terminal amide)
Molecular Formula C₂₂₅H₃₄₈N₄₈O₆₈
Molecular Weight ~4813.5 g/mol
CAS Number 2023788-19-2
Elimination Half-Life ~5 days (in vivo, human)
Solubility Bacteriostatic Water / Sterile Water
Primary Class Dual Incretin (GIP/GLP-1) Receptor Agonist

Biochemical Architecture & Mechanisms

1. Imbalanced Dual-Receptor Signaling Profile

Tirzepatide exhibits differential activation kinetics across its target receptors: it acts as a full agonist at the GIP receptor while showing biased, lower-potency signaling at the GLP-1 receptor that favors intracellular cAMP generation over β-arrestin recruitment.

2. Structural Protection & Albumin Binding

Steric protection provided by Aib at positions 2 and 13 prevents metabolic degradation by Dipeptidyl Peptidase IV (DPP-IV). The C₂₀ diacid side chain creates a prolonged depot effect through reversible albumin conjugation, reducing renal clearance rates.

3. Physiological Pathways

  • Insulin Secretion: Co-engages GIP and GLP-1 pathways on pancreatic beta cells to enhance glucose-dependent insulin secretion.
  • Satiety & Motility: Modulates hypothalamic anorectic signaling and slows gastric emptying kinetics in research models.

Nomenclature Note: Secondary marketing literature sometimes mislabels Tirzepatide as “GLP-2.” However, Tirzepatide exhibits no binding activity at GLP-2 receptors; it is classified exclusively as a GIP/GLP-1 dual receptor agonist.

For laboratory research, educational, and analytical reference only. Strictly not for human or veterinary use.

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