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

Cell Type:

U373 MG

Assay Information

Assay Type:

Functional

Assay Sub Type:

Cell Based

Functional Mode:

Agonist

Detection Method:

Fluorimetry

Measured Response:

Fluorescence

Testing Information

Incubation:

RT

Control Activator:

[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: 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

36511

Name

Substance P

Measurement

- EC50

PubChem ID

44338651

Name

[Sar9,Met(O2)11]-SP

Measurement

0.17nM - EC50

PubChem ID

57339975

Name

NKB [MePhe7]

Measurement

1200nM - EC50

PubChem ID

Name

[Nleu10]-NKA (4-10)

Measurement

433nM - EC50

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

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