Ligand-Gated Ion Channel Library

Ligand-gated ion channels (LGICs) are intact membrane proteins capable of carrying orthosteric binding sites for neurotransmitters and ion channels across membranes. LGICs can mediate intercellular communication by translating the binding of neurotransmitters released from the presynaptic terminal into an ion fluxes in the postsynaptic membrane. In addition to the recognized role of LGICs in neurotransmission, some LGICs are critical in non-excitable cells such as endothelial cells, suggestive of a broader functional role of these receptors outside the peripheral and central nervous system. LGICs are associated with several neurodegenerative diseases including Alzheimer's disease and Parkinson's disease, as well as epilepsy, hypertonic plexus disorder, and neuropathic pain, as they are characterized by major LGIC dysfunction. LGICs therefore represent attractive targets for new therapeutic agents.

In order to find attractive targets for new therapeutic agents with improved discrimination between receptor isoforms and a reduced propensity for off-target effects, BOC Sciences can design a novel ligand-gated ion channel library containing 4,000 compounds.

Figure 1. Structure of pentameric LGIC. (Nasiripourdori, A.; et al. 2011)

Library Design

1. Shape similarity
2. Topological similarity

Ligand-Gated Ion Channel Library Characteristics

• Favorable physicochemical parameters and solubility requirements
• No PAINS or toxic substances/unwanted functions: filtered by strict ‘Ro5-like’ physicochemical and most stringent in-house structural filters
• Bioactivity and safety confirmed by preclinical studies and clinical trials
• Structural diversity, medicinal activity, and cellular penetration
• Structural document, IC₅₀, and other chemical and biological data are provided
• All compounds are continually updated
• Compound cherry-picking service is provided

Figure 2. Structure of tetrameric LGIC. (Nasiripourdori, A.; et al. 2011)

What We Deliver

• Delivered within 2 weeks in any customer-preferred format
• Powders, dry films or DMSO solutions formatted in vials, 96 or 384-well plates
• All compounds have a minimum purity of 90% assessed by ¹H NMR and HPLC
• Analytical data is provided

BOC Sciences provides professional, rapid and high-quality services of Ligand-Gated Ion Channel Library design at competitive prices for global customers. Personalized and customized services of Ligand-Gated Ion Channel Library design can satisfy any innovative scientific study demands. Our clients have direct access to our staff and prompt feedback to their inquiries. If you are interested in our services, please contact us immediately!