Custom Radiolabeling

METIS Labs can provide you custom radiolabeling and custom radiosynthesis of your small molecules, peptides, and proteins.  METIS Labs’ will confidentially advise you on the appropriate labeling technique.  High specific activity and retention of the molecular structure is essential for the success of radiometric assays such as:

Receptor Ligand Binding
in vitro Autoradiography
ex vivo Autoradiography
in vivo receptor occupancy

Analysis of products is performed using methods including LC-MS, HPLC-Radiochemical Flow, HPLC-UV, TLC Radioscan and NMR.

Custom synthesis is an important part of our business.  Often we subsidize the cost of custom synthesis for potentially new catalog products. Many of our exclusive products in our radiochemical catalog have been derived from custom syntheses.  Built upon years of experience in a top pharmaceutical company our organic chemists provide world class expertise and integrated solutions to accelerate your drug development programs.

Please contact us by email or by phone (888.295.7550) to discuss how METIS Labs can rapidly fulfill you radiolabeling needs.

[125I] Radioiodination

METIS Labs Custom Radioiodination Services offers a wide range of labeling techniques to best maintain the biological activity of your molecule to advance your drug development pipeline.

Bolton-Hunter Reagent – Compounds containing Lysine Groups

Labels terminal amino groups with a radioiodinated phenolic residue, effectively introducing  radioactive iodine into proteins and peptides.  Since it is a non-oxidative technique, it is “less harsh” to proteins than alternative methods in turn retaining a high degree of binding activity to receptors.

Chloramine-T – Molecules containing Tyrosine or Histidine

Labels peptides and proteins naturally containing, or have been chemically modified, either tyrosine or histidine.  Hypochlorite released from chloramine-T acts as an effective oxidizing agent for iodide which undergoes electrophilic substitution to the tyrosine or histidine.

Lactoperoxidase –  Compounds containing Tyrosine

Lactoperoxidase catalyzes the oxidation of iodine using hyrdogen peroxide as a substrate.  It is a milder oxidative method than Iodogen® and leaves methionine residues intact

Iodogen® – Molecules containing Tyrosine or Histidine

This is an effective method for labeling a variety of proteins and peptides.  This oxidative method involves exposure of the substrate to Iodogen® in the presence of sodium [125I]Iodide followed by HPLC or other seperation techniques.  It produces high specific activity proteins or peptides in good yields.  However, a drawback is that cysteine and methionine residues in the peptide may be partially oxidized during the procedure.

Iodogen® is a registered trademark of Pierce

[3H] Tritiation & [14C] Carbon Synthesis

METIS Labs can perform custom tritiation and carbon synthesis of small molecules for receptor binding, receptor occupancy and QWBA assays.  The following techniques are available:

Tritiation – Bromine Compound

Small molecules containing a bromine compound can be labeled with tritium.  The bromine atom on a phenyl ring can be substituted with tritium.

Tritiation – Unsaturated Compound

Small molecules containing a reducible double bond can be labeled with tritium

Tritiation – Ketone-containing Compound

Ketone-containing compounds can be labeled by using tritium to reduce the ketone to an alcohol.

Carbon Synthesis –

Our capabilities include O & N methylation using [14C] methyl iodide or cyanation using potassium [14C]cyanide.  The resultant [14C]-labeled compound can be used for biodistribution or whole body autoradiography studies, but generally lack sufficient specific activity to be used for radioligand binding or receptor occupancy assays.

PET/SPECT Isotope Synthesis

METIS Labs Calverton laboratory can conduct [18F], [124I], [64Cu] and other PET isotope labeling for preclinical occupancy studies and probe development.  Scanning is performed using a Inveon multimodality PET/SPECT/CT scanner.