Sodium Ion Channel Library

In the central nervous system, voltage-gated sodium channels are responsible for the formation and conduction of neuronal action potentials, and they are essential membrane proteins for neurons. Sodium channels play a central role in physiology: they can rapidly transmit depolarizing impulses throughout cells and cellular networks, enabling the coordination of higher processes ranging from movement to cognition. Sodium ion channels are therefore considered to be an important component in nociception. The selective Nav1.7 channel blockers are important novel analgesics.

Aiming to discover new Nav1.7 channel blockers, BOC Sciences can design a novel sodium ion channel library using the knowledge of voltage-gated targeted library construction.

Figure 1. Schematic depictions of the Na channel α subunit. (Bourinet, E.; et al. 2014)

Sodium Ion Channel Library Design

We have employed a set of substructure queries and 2D-fingerprints based on common structural motifs and pharmacophores to search the CD BioScience HTS compounds collections. Our team has performed a comprehensive analysis of known sodium channel blockers and carefully selected more than 6,000 of the most promising drug-like structures.

• Our ion channel library is enriched with compounds that bear saturated backbones which can be frequently seen in the structures of other ion channel blockers
• Most of compounds are relatively flat aromatic cores
• Highly polar backbone fragments/moieties, such as CONH₂, SO₂NHR, polar heterocycles, etc
• Compounds are located right in the middle of drug-like chemical space

Figure 2. Subunit structure of voltage-gated sodium channels. (Catterall, W. A. 2012)

Our Strategies

1. Abundant fragments/scaffolds/motifs
2. Pharmacophore identification
3. 2D-fingerprints

Sodium 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

Table1. Physicochemical parameters for the BOC Sciences Sodium Ion Channel Library

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 Sodium Ion Channel Library design at competitive prices for global customers. Personalized and customized services of Sodium 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!