Biological Information
Background Information:
Orexins, also called hypocretins, are the common names given to a pair of highly excititory neuropeptide hormone. Two highly-related peptides (Orexin A and B) are produced by cleavage of a single precursor protein. Both peptides bind to two G-protein coupled receptors, orexin-1 (OX1) and orexin-2 (OX2). The orexin receptors are located predominantly in the hypothalamus and locus coeruleus, but are also found elsewhere in the CNS. The orexins have been linked to a range of physiological functions including the control of feeding and energy metabolism, modulation of neuroendocrine function, and regulation of the sleep-wake cycle. Orexin OX1 recetor antagonism may useful for the treatment of insomnia and obesity.
Family:
GPCR
Sub Family:
Orexin
Class:
Class A
Protein Name:
OX1
Uniprot Number:
O43613
Protein Aliases:
orexin receptor 1
Gene Name:
HCRTR1
Gene ID:
3061
Gene Aliases:
OX1R
Accession Number:
NM_001525
Organism:
Human
Construct Details:
Recombinant
Assay Information
Assay Type:
Biochemical
Assay Sub Type:
Binding
Detection Method:
Radiometric
Measured Response:
Scintillation
Testing Information
Ligand:
[125I]orexin-A
Ligand Kd (nM):
0.87
Ligand Concentration:
0.1 nM
Non Specific:
1 µM SB 334867
Incubation:
60 min at RT
Control Inhibitor:
orexin-A
Test Concentration / Dose:
Eurofins will provide IC/EC50 calculation if 5 or more concentrations are selected.
Test Sample Requirements:
Minimum for 1) Screen: 60 μl of 10 mM stock -OR- 1 mg (pre-weighed) for 10µM final testing. 2) Dose Response: 90 μl of 10 mM stock -OR- 1 mg (pre-weighed) for a top concentration at 10 µM.
Minimum Order Quantity:
2
Turnaround Time
Standard:
15 Business Days
Reference Compound Data
Clinical Relevance
Therapeutic Area:
Metabolic Diseases
Additional Information
Brand:
LeadHunter
Testing Location:
France - Celle L'Evescault
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