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

PubChem ID

4331799

Name

288150-92-5

Measurement

33nM - IC50

PubChem ID

6604926

Name

792173-99-0

Measurement

8nM - IC50

PubChem ID

44404987

Name

Orexin-B

Measurement

13nM - IC50

PubChem ID

56842143

Name

Orexin-A

Measurement

0.87nM - IC50

Clinical Relevance

Therapeutic Area:

Metabolic Diseases

Additional Information

Brand:

LeadHunter

Testing Location:

France - Celle L'Evescault

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