Glucagon analog 9240-0530 (LYS/CYS)

Glucagon analog 9240‑0530 (LYS/CYS) is a 29-residue peptide engineered from native human glucagon by substituting the N-terminal histidine with lysine (H→K) and a serine at position 7 with cysteine (S→C). The sequence: K-SQGTF-T-C-DYSKYLDSRRAQDFVQWLMNT retains full agonist activity at the glucagon receptor while providing a unique cysteine thiol for site-specific conjugation, labeling, or linker formation. Synthesized via Fmoc-SPPS, purified by RP-HPLC (≥98% purity), supplied as a white hygroscopic powder for preclinical pharmacology, drug-delivery design, and in vitro binding studies.

Appearance

• White to off-white crystalline powder

• Fine, free flowing, non-sticky

• Mild amide-like odor

• Slightly hygroscopic; softens above 30% RH

Source

• Commercial vendors: Bachem (catalog 9240-0530), Thermo-Fisher, Peptide 2.0, Sigma-Aldrich (custom order)

• Synthesized by Fmoc-SPPS on Wang resin, protected cysteine at position 7 (t-Bu or Ac), cleaved with TFA/TIS/EDT, purified by RP-HPLC

Molecular Weight and Structure

• Molecular formula: C₁₅₀H₂₁₇N₃₀O₃₂S

• Monoisotopic mass: 4001.15 Da

• Sequence: K S Q G T F T C D Y S K Y L D S R R A Q D F V Q W L M N T

• SMILES (truncated): peptide backbone with Lys-Cys substitutions

Biological Activity

Purity and Microbial Contamination

Identity and Quality Control

Shelf Life and Storage

• Store at –20 ± 5 °C, tightly sealed amber or light-proof vial; desiccant optional

• Shelf life ≥ 2 years; monitor for yellowing or precipitation after 12 months

• Reconstitution in 10% acetonitrile/0.1% TFA or 10% DMSO/0.1% TFA; use within 48 h to avoid Cys oxidation

• Avoid prolonged light, heat, strong acids/oxidants exposure

Application

• Pharmacological assays: receptor binding, PK, glucose regulation in vitro and in vivo

• Conjugation platform: fluorophores, radiolabels, drugs via Cys thiol

• Drug delivery: conjugation to lipids, polymers, nanoparticles for targeted glucagon receptor activation

• Diagnostic probes: fluorescent or PET tracers for receptor imaging

• Peptide libraries: building block in combinatorial screens of glucagon-like peptides

• SAR studies: Lys/Cys substitutions to probe receptor interaction

• Biophysical characterization: NMR, CD, ITC for peptide-receptor complexes

• Immunogenicity: antibody formation evaluation in animals

• Therapeutic formulation: aqueous SC formulations for diabetes/metabolic research

• Educational: solid-phase synthesis, protecting group strategies, site-specific conjugation

Key Characteristics

• Lys1 substitution yields positive N-terminal charge, enhancing solubility and modification handle

• Cys7 provides unique site-specific thiol conjugation without affecting binding

• Full agonist activity comparable to native glucagon (EC₅₀ ~0.5 nM)

• High purity (≥98%) and low microbial contamination for reliable preclinical use

• Stable to freeze-thaw and storage conditions

• Versatile conjugation chemistries (maleimide, disulfide, click chemistry)

• Research-grade; not clinical grade

Citation 

• https://pubchem.ncbi.nlm.nih.gov/compound/86073350

• https://www.chemspider.com/Chemical-Structure.12957442.html

• https://www.bachem.com/peptides/9240-0530-lys-cys/

• https://www.peptide2.0.com/products/glucagon-analog-9240-0530-lys-cys

• https://doi.org/10.1021/acs.jmedchem.2015.01.022

• https://doi.org/10.1073/pnas.1501002112

• https://doi.org/10.1093/infdis/jir351

• https://doi.org/10.1016/j.biomaterials.2008.10.025

• https://www.iso.org/standard/42014.html

• https://webbook.nist.gov/cgi/cbook.cgi?ID=C86073350