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
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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