Ion channels

Solute carrier family 12 member 5 (hKCC2)

CALIXAR’s hKCC2 (K-Cl cotransporter 2) aids in the exploration, advancement, and validation of new molecules as well as therapeutic antibodies. This membrane protein is ideal for neurological disorders including pain and epilepsy.This plasma membrane neuron-specific chloride potassium symporter is responsible for establishing the chloride ion gradient in neurons through the maintenance of low intracellular chloride concentrations.It is a critical mediator of synaptic inhibition, cellular protection against excitotoxicity and may also act as a modulator of neuroplasticity.Potassium chloride co-transporter 2 is a powerful therapeutic targets especially in the treatment of such conditions including pain and epilepsy.

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What makes us special

K-Cl cotransporter 2: We use a unique & custom-built approach to give us the edge

CALIXAR’s Solute carrier family 12 member 5 (hKCC2) facilitates reliable fragment-based drug design (FBDD), structure-based drug discovery (SBDD)and antibody discovery against this specific target.

Unlike Calixar’s hKCC2, other possible methods result in a potassium chloride cotransporter that becomes mutated and truncated (96 amino-acids at the C-terminus). In addition, this mutated version converts to a locked conformation within an antagonist.

As with all co-transporters and ion channels, hKCC2 membrane proteins are unstable targets and are difficult to produce natively with conventional procedures. Traditionally, the Solute carrier family 12 member 5 was never isolated from the membrane without causing aggregates due to its unstable construction.

Contrarily, Calixar’s co-transporters are the only original native and purified K-Cl cotransporter 2 on the market as it has been shown to be active in electrophysiology and thallium assays.

Our purified hKCC2 membrane protein can bind to antagonist compounds using SPR. This preparation permits the first functional architecture of hKCC2 reported up to date (Agez M. et al., 2017, Scientific Reports).

Our K-Cl cotransporter 2 maintains its structural and functional integrity and is purified and stabilized to full length and wild-type (native) protein. This membrane target has the ability to bind to an open and wide range of compounds including agonists, antagonists, and allosteric modulators.

Native Full-Length Proteins

CALIXAR’s hKCC2 is the first native full-length and functional target on the market. Other existing hKCC2 membrane targets are either mutated or truncated. Our hKCC2 membrane protein is produced in a eukaryotic system with the customary post-translational modifications (glycosylation), which gives us the ability to modify the buffer condition.

Specifically made for Biotech

CALIXAR’s K-Cl cotransporter 2 is a high-quality membrane protein used for pharmaceutical discovery and is adapted for use in biotechnology companies, or academic teams that are involved in the life science fields.

For any Life Science Project
  • Antibodies (including nanobodies, scaffold proteins, aptamers)
  • Small molecules
  • 3D Structures (classical X-ray or XFEL, Cryo-EM, NMR)
  • Drug discovery (Screening: HTS, FBDD, SBDD; Hit and lead validation)
  • Antibody discovery (Immunization and display technologies)
  • Clinical stage (drug validation on reliable native KCC2)​
More documentation

Solute carrier family 12 member 5 references

SCIENTIFIC REPORTS

Molecular architecture of potassium chloride co-transporter KCC2

Agez M et al. 2017
DISCOVERY ON TARGET

Towards Native and Stable GPCRs for Conformational Antibody Development

Jawhari A. Boston, 2015
ANALYTICAL BIOCHEMISTRY

Novel systematic detergent

Desuzinges Mandon E. et al. 2017

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Starting from native material or recombinant systems, we succeed with all types of membrane proteins: GPCRs, Ion Channels, Transporters, Receptors and Viral Proteins.