Biological Information

Background Information:

Corticotropin-releasing factor (CRF, interchangeable with corticotropin-releasing hormone, CRH) receptors belong to the superfamily of G protein-coupled seven transmembrane proteins. Two major subtypes of the CRF receptor have been termed the CRF1 and CRF2 receptors. The CRF1 receptor is abundantly expressed in the central nervous system with major expression sites in cortex, cerebellum, hippocampus, amygdala, olfactory bulb, and pituitary. CRF1 receptor antagonism may block stress-related responses and be useful in the treatment of anxiety, depression and gastrointestinal distress.

Family:

GPCR

Sub Family:

Corticotropin-Releasing Factor

Class:

Class B

Protein Name:

CRF1

Uniprot Number:

P34998

Protein Aliases:

CRF-R1|CRFR-1|Corticotropin-releasing hormone receptor 1|CRH-R-1|CRH-R1

Gene Name:

CRHR1

Gene ID:

1394

Gene Aliases:

CRF-R|CRF1

Accession Number:

NM_004382

Organism:

Human

Construct Details:

Recombinant

Assay Information

Assay Type:

Biochemical

Assay Sub Type:

Binding

Detection Method:

Radiometric

Measured Response:

Scintillation

Testing Information

Ligand:

[125I]sauvagine

Ligand Kd (nM):

0.12

Ligand Concentration:

0.075 nM

Non Specific:

0.5 µM Sauvagine

Incubation:

120 min at RT

Control Inhibitor:

sauvagine

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

177990

Name

antalarmin

Measurement

3nM - IC50

PubChem ID

16133798

Name

astressin

Measurement

2.4nM - IC50

PubChem ID

Name

sauvagine

Measurement

0.3nM - IC50

PubChem ID

Name

CRF

Measurement

3.1nM - IC50

Clinical Relevance

Therapeutic Area:

CNS/Addiction/Pain

Additional Information

Brand:

LeadHunter

Testing Location:

France - Celle L'Evescault

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