Purified Membrane Proteins

Melatonin receptor type 1A - Class A GPCR

CALIXAR’s MTR1A (Melatonin receptor type 1A) helps you identify, develop, and test new molecules and therapeutic antibodies for CNS neuroprotection treatments for insomnia, circadian sleep disorders, depression, cardiovascular regulation, cancer, and neurodegenerative diseases.

Melatonin receptor type 1A is a powerful therapeutic candidate for insomnia, circadian sleep disorders, depression, cardiovascular regulation, cancer, and neurodegenerative diseases.

Purchase Melatonin receptor type 1A - Class A GPCR

Our Melatonin receptor type 1A (MTR1A) is a class A GPCR that modulates neuronal firing, arterial vasoconstriction, cell proliferation in cancer cells, and reproductive and metabolic functions.

Target name: Melatonin receptor type 1A (MTR1A)

Gene: MTNR1A

Uniprot Accession: P48039

Origin: Human (Homo sapiens)

Class: Class A GPCR 

Sequence: Full-length, wildtype sequence, with a N-terminus Strep tag II, 8xHis-tag, and TEV protease cleavage site

Affinity Tag: Strepx2/His (both N-terminal)

Catalogue number: PP2

Theor. MW: 44,8kDa

Shipment temperature: Dry Ice

Storage conditions: Store at -80°C

Expression system: Sf9 insect cells (baculovirus)​

Purity: >90%

Purification: Metal Affinity Chromatography in presence of Sarkosyl/CHS

Activity: Confirmed by radiobinding assay and activation of Gi

Concentration​: Up to 5mg/ml

Sample buffer: 25mM Na2HPO4 pH 8.0, 150mM NaCl, 0.86%/0.18% Sarkosyl/CHS

Available quantity: From 10µg up to mg scale

€1,000.00 (10µg)

Ships in 7 business days

First in market

CALIXAR is the first to produce native, wild-type, unmutated and untruncated targets.

Better discovery

Develop reliable and effective drugs and antibodies as they are not locked in any specific conformation.

Why choose us?

Melatonin receptor type 1A: We apply a unique & custom-built program to give you an edge

Melatonin receptor type 1A (MTR1A)  modulates neuronal firing, arterial vasoconstriction, cell proliferation in cancer cells, and reproductive and metabolic functions.  MTR1A is a good therapeutic candidate for insomnia, circadian sleep disorders, depression, cardiovascular regulation, cancer, and neurodegenerative diseases.

CALIXAR’s  Melatonin receptor type 1A aids in reliable fragment-based drug design (FBDD), structure-based drug discovery (SBDD) and antibody discovery against this specific target. 

Unlike Calixar’s MTR1A, other alternative approaches have resulted in a Melatonin receptor that becomes mutated and truncated (96 amino-acids at the C-terminus). This truncation is unable to bind to its natural ligands. In addition, this mutated version becomes locked within an antagonist conformation.

As with all GPCRs, MTR1A is unstable target and inherently difficult to produce natively with conventional approaches. Traditionally, Melatonin receptor type 1A could only be locked in one specific conformation (e.g. antagonist) and were only ever developed in a solution that essentially cannot be pure, nor native (truncated, mutated), without PTMs, and consequently are unstable.

In contrast, CALIXAR’s MTR1A is able to bind to agonists, antagonists, as well as allosteric modulators and preserve their structural and functional integrity. They are purified and stabilized to full length and wild-type (native) proteins.

CALIXAR’s MTR1A is the first native full-length and operative target on the market. Other existing MTR1A targets are either mutated and or truncated. Our Melatonin receptor type 1A is produced in a eukaryotic arrangement with the precise post-translational adjustments (glycosylation).

CALIXAR’s MTNR1A Melatonin receptors are high-quality membrane proteins utilized in (bio)drug discovery projects and are adapted for use in pharmaceutical firms, biotechnology companies, as well as for academic teams that are committed to the life science fields.

  • Capacity to adapt the buffer condition
  • Antibodies (including nanobodies, scaffold proteins, aptamers)
  • Small molecules
  • 3D Structures (classical X-ray or XFEL, Cryo-EM, NMR)
  • Medicine discovery (Screening: HTS, FBDD, SBDD; Hit and lead validation)
  • Antibody discovery (Immunization and display technology)
  • Clinical stage (drug validation on reliable native MT1)

Melatonin receptor type 1A References

Molecular & Cellular Proteomics

Purification and identification of G protein-coupled receptor protein complexes under native conditions

Daulat AM. Et al. 2017 

Analytical Biochemistry

Novel systematic detergent screening method for membrane proteins solubilization.

Desuzinges Mandon E. et al. 2017

Membrane Protein Purchase

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