Biological Information

Background Information:

Prostanoid receptors 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. Prostanoid Thromboxane A2 (TP) receptors are present nearly all vascular and airway smooth muscle and blood platelets. TP receptor agonism may facilitate vascular, uterine and bronchial constriction, gastrointestinal spasm, allergic inflammation and platelet aggregation. TP receptor antagonism may be useful in the treatment of chronic productive cough, thrombosis, and atherosclerosis.

Family:

GPCR

Sub Family:

Prostanoid

Class:

Class A

Protein Name:

TP (TXA2)

Uniprot Number:

P21731

Protein Aliases:

Prostanoid TP receptor

Gene Name:

TBXA2R

Gene ID:

6915

Accession Number:

XM_011528214

Organism:

Human

Construct Details:

Recombinant

Cell Type:

HEK293

Assay Information

Assay Type:

Functional

Assay Sub Type:

Cell Based

Functional Mode:

Antagonist

Detection Method:

Fluorimetry

Measured Response:

Fluorescence

Testing Information

Incubation:

RT

Control Inhibitor:

SQ 29,548

Control Activator:

U 44069 (10 nM)

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

5311448

Name

SQ 29,548

Measurement

5.8nM - IC50

PubChem ID

24278225

Name

AL 8810

Measurement

8150nM - IC50

PubChem ID

329770690

Name

AH 6809

Measurement

30µM - IC50

PubChem ID

24724468

Name

Daltroban

Measurement

106nM - IC50

Clinical Relevance

Therapeutic Area:

Cardiovascular

Additional Information

Brand:

LeadHunter

Testing Location:

France - Celle L'Evescault

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