Biological Information

Background Information:

Tachykinins belong to the superfamily of G protein-coupled seven transmembrane proteins. G-protein-coupled receptors constitute one of the major signal transduction systems in eukaryotic cells. Coding sequences for these receptors, in those regions believed to contribute to the agonist-antagonist binding site, are strongly conserved across mammalian species. Tachykinin receptors are found in most peripheral tissue and within the central nervous system.

Family:

GPCR

Sub Family:

Tachykinin

Class:

Class A

Protein Name:

NK1

Uniprot Number:

P25103

Protein Aliases:

NK-1 receptor|NK-1R|Tachykinin receptor 1

Gene Name:

TACR1

Gene ID:

6869

Gene Aliases:

SPR|NK1R|NKIR|TAC1R

Accession Number:

NM_001058

Organism:

Human

Assay Information

Assay Type:

Biochemical

Assay Sub Type:

Binding

Detection Method:

Radiometric

Measured Response:

Scintillation

Testing Information

Ligand:

[125I]-Substance P LYS3

Ligand Kd (nM):

0.04

Ligand Concentration:

0.05 nM

Non Specific:

1 µM [Sar9,Met(O2)11]-SP

Incubation:

30 min at RT

Control Inhibitor:

[Sar9,Met(O2)11]-SP

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

44338651

Name

[Sar9,Met(O2)11]-SP

Measurement

0.29nM - IC50

PubChem ID

57339975

Name

NKB [MePhe7]

Measurement

2.2µM - IC50

PubChem ID

163828

Name

[Nle10]-NKA (4-10)

Measurement

4.8µM - IC50

Clinical Relevance

Therapeutic Area:

CNS/Addiction/Pain

Adverse / Beneficial Action:

Tachykinin receptor antagonism may find therapeutic use in the treatment of pain, emesis, inflammatory diseases and anxiety or depression.

Additional Information

Brand:

LeadHunter

Testing Location:

France - Celle L'Evescault

RELATED SOLUTIONS

Item: 2190
Item: 2192
Item: G085
Item: P22-p
Item: P3
Item: P342
Item: P9
Item: P363
Item: P411
Item: P426