Ion Channel Drug Discovery Assays and Products

Ion channels, which produce a gated, water-filled hole to assist in creating and modulating voltage potential across cell membranes, regulate the active transit of ions between the intracellular and extracellular environments. The ion channel family is closely involved in practically every area of physiology and is essential for a number of functions, including the relaxation of nerves and muscles, brain function, sensory transduction, blood pressure management, and cell growth. Their modulation has been connected to a variety of illnesses, such as blindness, kidney failure, neurological symptoms, cardiac problems, and neurological signs. It has been determined that over 60 human disorders known as "channelopathies" are caused by ion channel mutations. The ion channel superfamily is a promising potential target class for drug discovery due to the fundamental functional role it plays in human physiology, its membrane localization, and the variety of tissue distribution of its various members.

Fig.1 Ion channels. (Bagal, et al., 2013)

Creative Biolabs offers high-quality, innovative tools to help research groups accelerate ion channel drug discovery and development projects.

• Ion Channel Drug Discovery In Vitro Assays

Ion channels' ability to function normally is compromised by a variety of disorders, which has detrimental effects on the body. Ion channel and their modulator illnesses are brought on by autoimmune and genetic causes. Creative Biolabs offers ion channel in vitro assays to evaluate the therapeutic effects of your candidate against the targets of the membrane protein.

• Ion Channel Cell Lines

Researchers can identify ion channels, analyze chemicals, and find medications early on thanks to stable ion channel cell lines. We can more precisely study the mechanisms and functions of ion channels and find potential ion channel-targeting drug candidates by using cutting-edge technologies applied to the detection of electrical signals from ion channels, such as manual or automated electrophysiology, fluorescence, and RT-PCR.

• Ion Channel Membranes

Membrane preparations from Creative Biolabs are quality-assured frozen membranes from cells expressing recombinant or natural proteins. To evaluate receptor density and affinity, each batch of the receptor is subjected to rigorous quality control testing.

• Membrane Protein Tools

Creative Biolabs has developed a comprehensive list of membrane protein tools to support the development of antibodies and other therapeutics. We are dedicated to bringing more value to our clients by providing stock products, more technical resources and custom protein production services.

• Fluorescent Indicator and Reagents

Creative Biolabs produces a new generation of improved fluorescence indicators and reagents. For your research needs, we provide a variety of membrane-permeable and impermeable ion indicators that target Ca²⁺, Na⁺, K⁺, TI⁺, as well as other fluorescent dyes.

Pharmacology

In every type of tissue and cell in the human body, ion channels are expressed. Studies on the inheritance of relatively uncommon monogenic disorders brought on by mutations that interfere with the operation of particular ion channels have provided the most convincing evidence for a role in disease.

Phylogeny

Pore-forming ion channel family makes up about 1% of the estimated 20 000 human protein-coding genes and is larger than the nuclear hormone receptor family and roughly half the size of kinase and protease families in the human genome. The voltage-gated K_v potassium channels are covered by the family's main branch, and generally, potassium channels make up the largest percentage of the entire ion channel proteome. Members of the K_v branch of the family are considerably different from other potassium channels, such as the K2P or the Kir channels, in terms of sequence and topology.

Fig.2 Relative size of the ion channel and other protein families. (Bagal, et al., 2013)

Reference

1. Bagal, S.K.; et al. Ion channels as therapeutic targets: a drug discovery perspective. Journal of medicinal chemistry. 2013, 56(3): 593-624.