Celtarys expands its catalogue of receptor ligands with the first commercially available red-emitting fluorescent σ1/σ2 ligands

Sigma (σ) receptor subtypes, σ1 and σ2, are targets of wide pharmaceutical interest. σ1 receptor ligands are under evaluation in clinical trials for the treatment of diseases such as Alzheimer’s disease (AD), Huntington’s disease (HD) and neuropathic pain. Interest in the σ1 receptor as target for the development of anti-SARS-CoV-2 agents, and for the treatment of rare diseases has also lately emerged. On the other hand, σ2 receptor is overexpressed in a wide variety of tumors, so that it represents a target for the diagnosis and therapy of different tumor types. Importantly, an allosteric antagonist of the σ2 receptor is in clinical phases for the treatment of mild to moderate AD. 

However, despite this strong pharmacological interest, we lack commercial optimal chemical tools to study this class of receptors. To address this gap, Celtarys has reached a collaboration agreement with the University “Aldo Moro” of Bari to commercialize CELT-483, a potent σ1/σ2 receptor fluorescent ligand developed by the group of Prof. Carmen Abate, from the Department of Pharmacy-Pharmaceutical Sciences of this University.  

Abate and her colleagues are experts in the σ receptor subtypes field, and have been working in the development of fluorescent tools for these targets since 2007. Thanks to this agreement, Celtarys offers now to the scientific community the first red-emitting fluorescent σ2 ligand, that binds also to σ1. CELT-483 has been largely validated in fluorescence-based assays, among them flow cytometry and confocal and live cell microscopy (see Abatematteo et al., 2023, CELT-483 corresponds to compound 19). Moreover, to facilitate the performance of selective assays, we also offer kits with the σ1/σ2 receptor fluorescent ligand CELT-483 together with masking agents for σ1 (L6) or σ2 (F390) receptors.

More information and applications:

https://pubs.acs.org/doi/10.1021/acs.jmedchem.2c01227