Now on opnMe: BI-7150, a potent and selective voltage-gated Na+ channel 1.1 activator

20 January 2025

Voltage-gated Na⁺ channels (Na_v1.1 – Na_v1.9) are transmembrane proteins involved in the conduction of sodium ions and action potential initiation and propagation. They play a crucial role in the function of excitable tissues in the central nervous system, peripheral nervous system, heart, skeletal muscle, and nociceptive signaling. Based on human genetic data, loss-of-function mutations in specific Na_v channels can lead to severe neurological disorders, highlighting the need to maintain normal channel function. The Na_v1.1 channel, in particular, is essential for generating action potentials in inhibitory interneurons and regulating neuronal network synchronization and excitability, making drug-mediated increases in Na_v1.1 function an interesting biological concept. 

Accelerate your research on inhibitory GABAergic interneurons with our potent and selective voltage-gated Na⁺ channel 1.1 activator BI-7150. This molecule and its structurally related inactive analogue BI-7283, are now available free-of charge via opnMe and can be used to investigate the roles of Na_v1.1 in vitro. Interested researchers will receive the molecule free of charge and have full ownership of their results. We encourage you to publish your findings as part of our commitment to open science.

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About BI-7150:

BI-7150 is a potent small-molecule activator of voltage-gated Na⁺ channel Na_v1.1 that can be used for in vitro studies. The compound is representative of a structural class which is different from other known Na_v1.1 activators¹. BI-7150 shows good aqueous solubility and permeability as well as acceptable metabolic stability across human, rat, and mouse hepatocytes and a reduced protein binding. For your Na_v1.1 research, you can also order the structurally close analogue BI-7283 as a negative control.

About opnMe:

opnMe.com, the open innovation portal of Boehringer Ingelheim, fosters science and collaboration initiatives in areas of high unmet medical need. As part of our first pillar, the “Molecules to Order”, we share well-characterized tool compounds free of charge with no IP strings attached. These are complemented by “Molecules for Collaboration” where we offer access to unprecedented, often unpublished molecules, together with an attractive funding package. Interested scientists are invited to submit testable research hypotheses with these assets in novel diseases or combinations. With our “opn2EXPERTS” and “techMATCH” programs, we enlist scientific advice on key biologic issues to fuel further drug discovery and deliver novel solutions that benefit unmet patient needs. Our opn2TALENTS PostDoc grants, such as our recent call for proposals to optimize a poxvirus-based cancer vaccine platform, provide an opportunity for high-caliber talents to pitch their scientific approaches for well-defined research questions to conduct their research at one of our discovery research sites.