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:

Full Length, Recombinant

Cell Type:

CHO-K1

Assay Information

Assay Type:

Functional

Assay Sub Type:

Cell Based

Functional Mode:

Agonist

Detection Method:

TR-FRET

Measured Response:

Fluorescence

Testing Information

Incubation:

30 min at 37°C

Control Activator:

GR 64349

Criteria For Significance:

≥ 50% increase in IP-one relative to GR 64349 response, ≥ 50% Inhibition of GR 64349-induced response

Test Concentration / Dose:

Compounds are screened at 10, 3, 1, 0.3, 0.1, 0.03, 0.01 and 0.003 μM

Test Sample Requirements:

75 μl of 10 mM stock or 1 mg (pre-weighed) powder (assuming FW ≦500 and purity 100%)

Minimum Order Quantity:

16

Turnaround Time

Standard:

20 Business Days

Reference Compound Data

PubChem ID

5311135

Name

CHEMBL131872

Measurement

0.069μM - EC50

Clinical Relevance

Therapeutic Area:

CNS/Addiction/Pain

Adverse / Beneficial Action:

Tachykinin receptor agonism may result in vasodilation, salivary and mucous secretion, emesis, brochoconstriction, micturation, modulate behavior, increase pain transmission and neurogenic inflammation. 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:

Taiwan - Taipei

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