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Cagrilintide

Identification

Property Value
Class Long-acting amylin analog
Molecular Weight ~4,433 Da
Appearance White to off-white lyophilized powder
Solubility Soluble in aqueous buffers at physiological pH
Receptor Target Amylin receptor (AMY1, AMY3 subtypes); calcitonin receptor (CTR) complex with RAMP1/RAMP3
Half-Life ~7–10 days (engineered for weekly administration via lipidation and amino acid substitutions)

Structural & Pharmacological Profile

Cagrilintide is a synthetic amylin analog engineered for extended pharmacokinetics. Native amylin is a 37-amino acid peptide co-secreted with insulin from pancreatic β-cells. Cagrilintide incorporates structural modifications that confer resistance to proteolytic degradation and high-affinity albumin binding, extending its half-life from the native ~13 minutes to approximately 7–10 days.

Key Structural Features

Feature Detail
Parent Molecule Human amylin (islet amyloid polypeptide, IAPP)
Half-Life Extension Achieved through lipidation (fatty acid conjugation for albumin binding) and non-proteinogenic amino acid substitutions
Amyloidogenicity Reduction Amino acid substitutions in the amyloidogenic region (residues 20–29) prevent fibril formation, a known limitation of native amylin
Albumin Binding Reversible, high-affinity binding to serum albumin reduces renal clearance

Research Applications

Research Domain Description
Satiety & Appetite Regulation Amylin receptor activation in the area postrema (hindbrain) induces meal-ending satiety signals; reduces meal size and frequency
Gastric Emptying Dose-dependent slowing of gastric emptying rate, prolonging postprandial nutrient delivery and enhancing satiety signaling
Glucagon Suppression Suppresses postprandial glucagon secretion, reducing hepatic glucose output
Combination with GLP-1R Agonists Investigated in combination with semaglutide (CagriSema); additive or synergistic effects on body weight and glycemic control observed in Phase 2 studies
Body Weight Management Weight reduction driven primarily by reduced energy intake rather than increased expenditure; distinct mechanism from GLP-1R agonists

Quality Specifications

Parameter Specification Method
Purity (HPLC) ≥99.0% RP-HPLC, 214 nm
Mass Identity MW ±1.0 Da ESI-MS
Water Content ≤5.0% Karl Fischer titration
Peptide Content ≥80.0% Amino acid analysis
Counterion Acetate (≤1.0% TFA) Ion chromatography
Endotoxin ≤1.0 EU/mg LAL kinetic chromogenic
Residual Solvents ≤ ICH Q3C limits Headspace GC
pH (1 mg/mL) 5.0–7.5 Potentiometric

Available Configurations

Format Size Vials per Kit
Standard Research Kit 5 mg × 10 vials 10
Extended Research Kit 10 mg × 10 vials 10
Custom Configuration Per project requirements Per scope

Storage & Stability

Condition Requirement
Short-term Storage 2–8°C, lyophilized form
Long-term Storage −20°C to −80°C, desiccated
Reconstituted 24 h at 2–8°C; aliquot and freeze at −20°C for extended use
Shipping Cold chain (2–8°C) recommended; ambient ≤7 days

Documentation

  • COA per batch: HPLC purity chromatogram, ESI-MS spectrum, quantitative data
  • MSDS per shipment

Special Notes

  • FOR LABORATORY RESEARCH USE ONLY.
  • Unlike native amylin, cagrilintide is engineered to have minimal fibrillogenic potential. However, researchers should avoid reconstitution in acidic buffers (pH < 4.0) as this may promote aggregation over extended incubation periods.
  • Amylin receptor pharmacology is complex due to CTR/RAMP heterodimerization. In vitro binding assays should consider the specific AMY receptor subtype (AMY1 vs AMY3) under investigation.
  • For combination studies (e.g., cagrilintide + semaglutide), reconstitute each peptide separately and prepare fresh mixtures immediately before use to avoid potential peptide-peptide interactions in solution.

Key Research References

Reference PMID Key Finding
Enebo LB et al. "Safety, tolerability, pharmacokinetics, and pharmacodynamics of concomitant administration of multiple doses of cagrilintide with semaglutide 2.4 mg for weight management: a randomised, controlled, phase 1b trial." Lancet. 2021;397(10286):1736–1748. 33894838 Cagrilintide + semaglutide (CagriSema) combination demonstrated additive weight loss with tolerable safety profile; established dual amylin/GLP-1 approach
Frias JP et al. "Efficacy and safety of co-administered cagrilintide 2.4 mg and semaglutide 2.4 mg (CagriSema) once weekly in type 2 diabetes: a multicentre, phase 2, randomised controlled trial." Lancet. 2023;402(10403):720–730. 37364590 Phase 2 T2D trial: CagriSema produced superior HbA1c and body weight reductions vs semaglutide alone, confirming amylin/GLP-1 additive pharmacology
Kruse T et al. "NN1213 - A Potent, Long-Acting, and Selective Analog of Human Amylin." J Med Chem. 2024;67(18):16867–16884. 38960379 Structural engineering of cagrilintide (NN1213) including lipidation for albumin binding and amino acid substitutions to eliminate amyloidogenicity of native amylin

Stability & Storage

Condition Degradation Profile
Lyophilized Storage Standard lyophilized peptide stability. 24 months at 2–8°C, 36 months at −20°C. Desiccated environment essential
Neutral pH (5.0–7.5) Stable; recommended for reconstitution and working solutions
Acidic pH (<4.0) May promote aggregation over extended incubation; avoid reconstitution in acidic buffers. Native amylin is known to aggregate at low pH
Alkaline pH (>8.0) Risk of deamidation and loss of receptor binding affinity
Temperature Stress The fatty acid conjugate is hydrophobic; mild aggregation possible with temperature fluctuations. Gentle agitation during reconstitution recommended
Reconstituted Solution 24 h at 2–8°C; aliquot and freeze at −20°C for ≤30 days. Avoid repeated freeze-thaw

Frequently Asked Questions

Q: What purity specifications apply to cagrilintide?

≥99.0% by HPLC at 214 nm with ESI-MS mass identity confirmation (±1.0 Da). Comprehensive QC includes peptide content (≥80.0%), water content (≤5.0%), counterion analysis (acetate, ≤1.0% TFA), and endotoxin testing (≤1.0 EU/mg). Unlike native amylin, cagrilintide's engineered substitutions reduce fibrillogenic potential — but every batch is monitored for aggregation. Full batch-specific COA included.

Q: How should cagrilintide be stored after reconstitution?

Reconstituted cagrilintide is stable for 24 hours at 2–8°C. For longer storage, aliquot into single-use portions and freeze at −20°C (stable ≤30 days). Avoid reconstitution in acidic buffers (pH < 4.0) which may promote aggregation despite the engineered reduction in amyloidogenicity. For combination studies with semaglutide, prepare fresh mixtures immediately before use. Avoid repeated freeze-thaw cycles.

Source & Purchase

For researchers requiring CAGRILINTIDE with full analytical documentation including HPLC and LC-MS traces, visit the PeptideSourceHub product page for bulk pricing and specifications.

Purchase CAGRILINTIDE with COA →

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