Tirzepatide

40MG per vial

Tirzepatide is a synthetic 39-residue peptide built on the GIP sequence scaffold and engineered for agonism at both the GIP receptor and the GLP-1 receptor, two class B G protein-coupled receptors. Alpha-aminoisobutyric acid substitutes for the native alanine residues at positions 2 and 13, conferring resistance to dipeptidyl peptidase-4 and constraining the helical conformation, while Lys20 carries a C20 fatty diacid attached through a gamma-glutamate and two 8-amino-3,6-dioxaoctanoic acid linkers, which drives albumin binding. Its pharmacology is both imbalanced and biased: engagement of GIPR is greater than that of GLP-1R, and at GLP-1R it favours cAMP generation over beta-arrestin recruitment, with correspondingly weaker receptor internalisation and desensitisation than native GLP-1.

Metabolic Signalling Endocrine Axis

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Research use only. Supplied for in vitro laboratory research. Not a drug, supplement, cosmetic or medical device, not approved by the TGA, and not for administration to humans or animals. See our research use conditions.

Compound signature

From confirmed structure

4814g/mol

Molar mass

341atoms

Heavy atoms

Atomic composition

C225H348N48O68

C225
H348
N48
O68

Characterised targets

GIPR
GLP-1R

Sequence

Y-Aib-EGTFTSDYSI-Aib-LDKIAQKAFVQWLIAGGPSSGAPPPS-NH2 (Aib at positions 2 and 13; Lys20 bears the C20 diacid conjugate)

Research applications

Cell-based signalling studies have quantified cAMP accumulation, beta-arrestin recruitment and receptor internalisation at recombinant human GIPR and GLP-1R, and cryo-electron microscopy with molecular dynamics has mapped the determinants of dual engagement, attributing the GLP-1R bias to a composite effect on signalling efficacy of the N-terminal tyrosine and the C20 diacid moiety. Islet studies have used receptor antagonism and knockout tissue to separate the two arms: in mouse islets the insulin secretory response is carried predominantly through GLP-1R because affinity and potency at the murine GIPR are several-fold weaker than for mouse GIP, whereas in human islets antagonising GIPR reduces the insulin response. Adipocyte work has examined GIPR-dependent regulation of nutrient handling in the fasted and post-prandial states, GIPR being expressed in adipocytes where GLP-1R is not.

Formulation and handling

The C20 diacid makes this peptide markedly more surface-active than unlipidated incretin analogues and prone to aggregation at air-liquid interfaces, so direct the diluent down the vial wall and dissolve by gentle swirling rather than shaking or vortexing. Solubility is poor near the isoelectric point; a near-neutral to slightly alkaline aqueous buffer dissolves it more cleanly than plain acidified water.

Intended use

Tirzepatide is supplied exclusively for in vitro and non-clinical scientific research. It is not approved for human or animal therapeutic, diagnostic or medicinal use. All handling and experimentation must be carried out by trained personnel in an appropriately controlled laboratory.

Specification

Presentation: Vial
Labelled strength: 40MG
Molecular formula: C225H348N48O68
Molar mass: 4813.5 g/mol
CAS number: 2023788-19-2
Molecular targets: GIPR, GLP-1R
Appearance: Lyophilised powder
Storage: 2–8 °C sealed, −20 °C long term

Values describe the compound as supplied. Analytical figures for the material in your vial are on that lot’s certificate, not here.

Certificates of analysis

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