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 OX2 receptor antagonism may be useful for the treatment of insomnia and obesity.

Family:

GPCR

Sub Family:

Orexin

Class:

Class A

Protein Name:

OX2

Uniprot Number:

O43614

Protein Aliases:

orexin receptor 2

Gene Name:

HCRTR2

Gene ID:

3062

Gene Aliases:

OX2R

Accession Number:

XM_017010798

Organism:

Human

Construct Details:

Recombinant

Cell Type:

HEK293

Assay Information

Assay Type:

Functional

Assay Sub Type:

Cell Based

Functional Mode:

Antagonist

Detection Method:

Fluorimetry

Measured Response:

Fluorescence

Testing Information

Incubation:

RT

Control Inhibitor:

JNJ-10397049

Control Activator:

orexin-B (30 nM)

Test Concentration / Dose:

Eurofins will provide IC/EC50 calculation if 5 or more concentrations are selected.

Test Sample Requirements:

Minimum for 1) Screen: 70 µL of 10 mM stock -OR- 1 mg (pre-weighed) for 10µM finµL 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:

16

Turnaround Time

Standard:

15 Business Days

Reference Compound Data

PubChem ID

9869934

Name

JNJ-10397049

Measurement

54nM - IC50

Clinical Relevance

Therapeutic Area:

CNS/Addiction/Pain

Additional Information

Brand:

LeadHunter

Testing Location:

France - Celle L'Evescault

RELATED SOLUTIONS

Item: 1988
Item: 2349
Item: G093