1027359-40-5

Upstream product

• 223742-32-3 1-N-chloroacetyl-2-N'-Cbz(ethylenediamine) 
• 122555-91-3 1,4,7-tris-tert-butoxycarbonylmethyl-1,4,7,10-tetraazacyclododecane 
• 294-90-6 1,4,7,10-tetraazacyclododecan 
• 72080-83-2 2-benzyloxycarbonylaminoethylamine 
• 1027359-36-9 N-(2-benzyloxycarbonylaminoethyl)bromoacetamide 

Relevant academic research and scientific papers

Optimization of Artificial Siderophores as 68Ga-Complexed PET Tracers for in Vivo Imaging of Bacterial Infections

The diagnosis of bacterial infections at deep body sites benefits from noninvasive imaging of molecular probes that can be traced by positron emission tomography (PET). We specifically labeled bacteria by targeting their iron transport system with artificial siderophores. The cyclen-based probes contain different binding sites for iron and the PET nuclide gallium-68. A panel of 11 siderophores with different iron coordination numbers and geometries was synthesized in up to 8 steps, and candidates with the best siderophore potential were selected by a growth recovery assay. The probes [68Ga]7 and [68Ga]15 were found to be suitable for PET imaging based on their radiochemical yield, radiochemical purity, and complex stability in vitro and in vivo. Both showed significant uptake in mice infected with Escherichia coli and were able to discern infection from lipopolysaccharide-triggered, sterile inflammation. The study qualifies cyclen-based artificial siderophores as readily accessible scaffolds for the in vivo imaging of bacteria.

Synthesis of a DOTA-C-glyco bifunctional chelating agent and preliminaryin vitroandin vivostudy of [68Ga]Ga-DOTA-C-glyco-RGD

The design of bifunctional chelating agents (BFCA) allowing straightforward radiometal labelling of biomolecules is a current challenge. We report herein the development of a bifunctional chelating agent based on a DOTA chelator linked to aC-glycosyl compound, taking advantage of the robustness and hydrophilicity of this type of carbohydrate derivative. This new BFCA was coupled with success by CuAAC with c(RGDfK) for αvβ3integrin targeting. As attested byin vitroevaluation, the conjugate DOTA-C-glyco-c(RGDfC) demonstrated high affinity for αvβ3integrins (IC50of 42 nM). [68Ga]Ga-DOTA-C-glyco-c(RGDfK) was radiosynthesized straightforwardly and showed high hydrophilic property (log?D7.4= ?3.71) andin vitrostability (>120 min). Preliminaryin vivoPET study of U87MG engrafted mice gave evidence of an interesting tumor-to-non-target area ratio. All these data indicate that [68Ga]Ga-DOTA-C-glyco-c(RGDfK) allows monitoring of αvβ3expression and could thus be used for cancer diagnosis. The DOTA-C-glycoside BFCA reported here could also be used with various ligands and chelating other (radio)metals opening a broad scope of applications in imaging modalities and therapy.

A bifunctional chelator featuring the DOTAM-Gly-l-Phe-OH structural subunit: en route toward homo- and heterobimetallic lanthanide(III) complexes as PARACEST MRI contrast agents

A new synthesis of a bifunctional chelator possessing DOTAM-Gly-l-Phe-OH and DO3A chelating cages interconnected by an oligoamide chain has been achieved via HBTU-mediated coupling from easily accessible building blocks. Both homo- and heterobimetallic lanthanide(III) complexes derived from this bifunctional chelator have been prepared in moderate yields. The CEST spectrum acquired for homobimetallic Eu3+ complex showed this molecule to be a promising PARACEST MRI contrast agent whereas the Eu3+/Tm3+ heterobimetallic complex lacked a useful CEST signal.

Bifunctional ligands based on the DOTA-monoamide cage

Efficient routes to DOTA-monoamide ligands bearing amino, hydroxyl, aldehyde and maleimido groups are described. These functional groups, which can be spaced at will from the coordination cage, will readily react with suitable groups of targeting moieties