Cagrilintide (Research Overview)
Cagrilintide is a synthetic, lipidated (fatty-acid-conjugated) analogue of amylin, a 37-amino-acid peptide hormone also known as islet amyloid polypeptide. It was described in the medicinal-chemistry literature as a stable, long-acting amylin analogue, developed from a starting point that is difficult to work with because native amylin readily forms amyloid fibrils.
Mechanism of Action
Amylin receptors are heteromeric G protein-coupled receptors. They form when the calcitonin receptor (CTR) associates with a receptor activity-modifying protein (RAMP), giving multiple receptor subtypes that are conventionally designated AMY1 to AMY3. The pharmacology of these multimeric receptors, including their affinity for amylin and for related peptides such as calcitonin gene-related peptide (CGRP), has been reviewed in the literature.
Cagrilintide is an analogue of the endogenous ligand. The primary report describes the structure-activity work that led to its selection, including the use of lipidation to produce a long-acting analogue, and compares it with the earlier amylin analogue pramlintide, which has a short half-life. Structural studies of related amylin receptor complexes (for example AMY1 bound to CGRP and Gs protein) provide molecular context for how peptide ligands engage CTR-RAMP assemblies.
Research Areas
Receptor pharmacology: amylin-family peptides are characterized in cell-based systems that express the calcitonin receptor with individual RAMPs, where ligand affinity and signalling are compared across receptor subtypes.
Peptide design and stability: cagrilintide is cited as an example of applying lipidation to an aggregation-prone peptide hormone, and amylin structure-function relationships and mimetic design are discussed in the reviews listed below.
Background literature: reviews of amylin biology and pharmacology describe the hormone and its receptors in rodents and in humans, and place analogues such as cagrilintide in that context.
Findings from published studies do not establish safety or efficacy for any indication and should not be interpreted as medical claims.
Specification summary
Cagrilintide 10mg
Stated purity ≥99%. For laboratory research use only.
Related materials
References
- Kruse T, Hansen JL, Dahl K, Schäffer L, Sensfuss U, Poulsen C, et al. Development of Cagrilintide, a Long-Acting Amylin Analogue. J Med Chem. 2021;64(15):11183-11194. PMID 34288673 · DOI
- Hay DL, Chen S, Lutz TA, Parkes DG, Roth JD. Amylin: Pharmacology, Physiology, and Clinical Potential. Pharmacol Rev. 2015;67(3):564-600. PMID 26071095 · DOI
- Bower RL, Hay DL. Amylin structure-function relationships and receptor pharmacology: implications for amylin mimetic drug development. Br J Pharmacol. 2016;173(12):1883-98. PMID 27061187 · DOI
- Poyner DR, Sexton PM, Marshall I, Smith DM, Quirion R, Born W, et al. International Union of Pharmacology. XXXII. The mammalian calcitonin gene-related peptides, adrenomedullin, amylin, and calcitonin receptors. Pharmacol Rev. 2002;54(2):233-46. PMID 12037140 · DOI
- Cao J, Belousoff MJ, Danev R, Christopoulos A, Wootten D, Sexton PM. Cryo-EM Structure of the Human Amylin 1 Receptor in Complex with CGRP and Gs Protein. Biochemistry. 2024;63(9):1089-1096. PMID 38603770 · DOI
Cited literature is provided for scientific context only and does not describe or endorse any use of these products.
For laboratory research use only. Not for human or veterinary use. Not intended to diagnose, treat, cure, or prevent any disease.