Biological Information

Background Information:

The cysteinyl leukotrienes (LTC4, LTD4, LTE4) are products of arachidonic acid metabolism and are released from various cells, including mast cells and eosinophils. These eicosanoids bind to cysteinyl leukotriene (CysLT) receptors. CysLT receptors belong to the superfamily of G protein-coupled seven transmembrane proteins. CysLT type-2 (CysLT2) receptor is found in lung macrophages, airway smooth muscle, cardiac Purkinje cells, adrenal medulla cells, peripheral blood leukocytes, spleen, placenta, and brain. CysLT2 is less well defined due to a lack of specific agonists and antagonists. Cysteinyl leukotriene antagonists may be therapeutically useful in the treatment of allergic-induced inflammation associated with asthma, rhinitis, pruritis, etc.

Family:

GPCR

Sub Family:

Leukotriene

Class:

Class A

Protein Name:

CysLT2

Uniprot Number:

Q9NS75

Protein Aliases:

G-protein coupled receptor GPCR21|hGPCR21|G-protein coupled receptor HG57|HPN321

Gene Name:

CYSLTR2

Gene ID:

57105

Gene Aliases:

CysLT(2)|CYSLT2R|CYSLT2|PSEC0146

Accession Number:

NM_001308468

Organism:

Human

Construct Details:

Recombinant

Assay Information

Assay Type:

Biochemical

Assay Sub Type:

Binding

Detection Method:

Radiometric

Measured Response:

Scintillation

Testing Information

Ligand:

[3H]LTD4

Ligand Kd (nM):

1.5

Ligand Concentration:

1 nM

Non Specific:

1 µM LTD4

Incubation:

60 min at RT

Control Inhibitor:

leukotriene C4

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

5280493

Name

Leukotriene C4

Measurement

4.74nM - IC50

PubChem ID

16760569

Name

MK 571

Measurement

11000nM - IC50

PubChem ID

5280878

Name

Leukotriene D4

Measurement

2.6nM - IC50

PubChem ID

5280492

Name

Leukotriene B4

Measurement

- IC50

Clinical Relevance

Therapeutic Area:

Inflammation/Allergy

Additional Information

Brand:

LeadHunter

Testing Location:

France - Celle L'Evescault

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