CysLT1 Human Leukotriene GPCR Cell Based Antagonist IP1 LeadHunter Assay - TW

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OVERVIEW

DOCUMENTS/REFERENCES

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-1 (CysLT1) receptor is found in the human airway and on other pro-inflammatory cells.

Family:

GPCR

Sub Family:

Leukotriene

Class:

Class A

Protein Name:

CysLT1

Uniprot Number:

Q9Y271

Gene Name:

CYSLTR1

Gene ID:

10800

Gene Aliases:

CysLT1|CysLT(1)|CYSLT1R

Accession Number:

NM_006639

Organism:

Human

Construct Details:

Full Length, Recombinant

Cell Type:

CHO-K1

Assay Information

Assay Type:

Functional

Assay Sub Type:

Cell Based

Functional Mode:

Antagonist

Detection Method:

TR-FRET

Measured Response:

Fluorescence

Testing Information

Incubation:

30 min at 37°C

Control Inhibitor:

MK 571

Criteria For Significance:

≥ 50% increase in IP-one relative to LTD4 response, ≥ 50% inhibition of LTD4-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:

Turnaround Time

Standard:

20 Business Days

Reference Compound Data

PubChem ID

16760569

Name

MK 571

Measurement

0.00072μM - IC50

Clinical Relevance

Therapeutic Area:

Inflammation/Allergy

Additional Information

Brand:

LeadHunter

Testing Location:

Taiwan - Taipei