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. The DP1 prostanoid receptor is activated by prostaglandin D2 (PGD2) and it is expressed in vascular smooth muscle, platelets, retina and hematopoietic cells. Activation of DP1 results in inhibition of platelet activation and vasodilation; they are also involved in sleep regulation. Prostanoid DP1 receptors may also play a role in immune and inflammatory responses. The potential therapeutic utilities of DP1 receptor agonists are for glaucoma, atopic dermatitis and antagonist for dyslipidemia and asthma, respectively.

Family:

GPCR

Sub Family:

Prostanoid

Class:

Class A

Protein Name:

DP1

Uniprot Number:

Q13258

Gene Name:

PTGDR

Gene ID:

5729

Gene Aliases:

DP|DP1|PTGDR1

Accession Number:

NM_000953

Organism:

Human

Construct Details:

Recombinant

Assay Information

Assay Type:

Biochemical

Assay Sub Type:

Binding

Detection Method:

Radiometric

Measured Response:

Scintillation

Testing Information

Ligand:

[3H]PGD2

Ligand Kd (nM):

1.2

Ligand Concentration:

1.5 nM

Non Specific:

1 µM BW245C

Incubation:

60 min at RT

Control Inhibitor:

BW 245C

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

119304

Name

BW 245C

Measurement

2.3nM - IC50

PubChem ID

119461

Name

AH 6809

Measurement

1133nM - IC50

PubChem ID

122021

Name

BW A868C

Measurement

16.7nM - IC50

PubChem ID

448457

Name

Prostaglandin D2

Measurement

3.1nM - IC50

Clinical Relevance

Therapeutic Area:

CNS/Addiction/Pain

Adverse / Beneficial Action:

Prostanoid DP receptor agonism may increase nociception, eosinophil recruitment in asthma and inhibit platelet aggregation. DP receptor antagonism may be useful in the treatment of allergic diseases and nociception as well as prolong bleeding time.

Additional Information

Brand:

LeadHunter

Testing Location:

France - Celle L'Evescault

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