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:

NK2

Uniprot Number:

P21452

Protein Aliases:

NK-2 receptor|NK-2R|Neurokinin A receptor|Tachykinin receptor 2

Gene Name:

TACR2

Gene ID:

6865

Gene Aliases:

SKR|NK2R|NKNAR|TAC2R

Accession Number:

NM_001057

Organism:

Human

Construct Details:

Recombinant

Assay Information

Assay Type:

Biochemical

Assay Sub Type:

Binding

Detection Method:

Radiometric

Measured Response:

Scintillation

Testing Information

Ligand:

[125I]NKA

Ligand Kd (nM):

0.12

Ligand Concentration:

0.1 nM

Non Specific:

300 nM [Nleu10]-NKA (4-10)

Incubation:

60 min at RT

Control Inhibitor:

[Nleu10]-NKA (4-10)

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:

10 Business Days

Reference Compound Data

PubChem ID

104974

Name

Saredutant

Measurement

0.29nM - IC50

PubChem ID

44338651

Name

[Sar9,Met(O2)11]-SP

Measurement

590nM - IC50

PubChem ID

57339975

Name

NKB [MePhe7]

Measurement

2700nM - IC50

PubChem ID

Name

[Nleu10]-NKA (4-10)

Measurement

5.38nM - 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

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