MT1 Melatonin receptors 1 are powerful therapeutic candidates for insomnia, circadian sleep disorders, depression, cardiovascular regulation, cancer, and neurodegenerative diseases.
CALIXAR’s MT1 (Melatonin receptor 1) 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.
CALIXAR's Melatonin receptor 1 (MT1) is a class A GPCR that modulates neuronal firing, arterial vasoconstriction, cell proliferation in cancer cells, and reproductive and metabolic functions.
Information
Target name: Melatonin receptor type 1A (MT1)
Catalogue number: PP2
Class: GPCR Class A
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)
Origin: Human (Homo sapiens)
Theor. MW: 44,8kDa
Accession #: P48039 (UniProt)
Shipment temperature: Dry Ice
Storage conditions: Store at -80°C
Production
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
CALIXAR applies a unique & custom-built program to give you an edge
Melatonin receptor 1 (MT1) is a class A GPCR that modulates neuronal firing, arterial vasoconstriction, cell proliferation in cancer cells, and reproductive and metabolic functions. MT1 is a good therapeutic candidate for insomnia, circadian sleep disorders, depression, cardiovascular regulation, cancer, and neurodegenerative diseases.
CALIXAR’s MT1 Melatonin receptors aid in reliable fragment-based drug design (FBDD), structure-based drug discovery (SBDD) and antibody discovery against this specific target.
Unlike Calixar’s MT1 Melatonin receptors, 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, MT1 Melatonin receptors are unstable targets and inherently difficult to produce natively with conventional approaches. Traditionally, MT1 Melatonin receptors 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 MT1 Receptors are 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.
Native Full-Length Proteins
CALIXAR’s MT1 Melatonin receptor 1 is the first native full-length and operative target on the market. Other existing MT1 targets are either mutated and or truncated. Our MT1 protein is produced in a eukaryotic arrangement with the precise post-translational adjustments (glycosylation).
Specifically Made for Biotech
CALIXAR’s MT1 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.
For Any Life Science Project
- 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)
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