CysLT1 Human Leukotriene GPCR Cell Based Agonist & Antagonist IP1 LeadHunter Assay - TW
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. These receptor antagonists are available for the treatment in inflammatory diseases, in particular asthma.
No. of Assays on Panel:
2
Assays on Panel:
Family
GPCR
Name
CysLT1 Human Leukotriene GPCR Cell Based Agonist IP1 LeadHunter Assay - TW
Item
331600-0
Protein
CysLT1
Organism
Human
Assay Sub Type
Cell Based
Family
GPCR
Name
CysLT1 Human Leukotriene GPCR Cell Based Antagonist IP1 LeadHunter Assay - TW
Item
331600-1
Protein
CysLT1
Organism
Human
Assay Sub Type
Cell Based
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:
Agonist & Antagonist
Detection Method:
TR-FRET
Measured Response:
Fluorescence
Testing Information
Procedure Summary:
Human CysLT₁ receptors expressed in CHO-K1 cells are used. Test compound and/or vehicle is incubated with the cells (1 x 10⁶ cells/ml) in stimulation buffer of IP₁ Gq detection kit for 30 minutes at 37 °C. Test compound-induced increase of IP₁ by 50 percent or more (≥50%) relative to the 1 μM LTD₄ response indicates possible CysLT₁ receptor agonist activity. Test compound-induced inhibition of 0.06 μM LTD₄-induced increase of IP₁ response by 50 percent or more (≥50%) indicates receptor antagonist activity.
Incubation:
30 min at 37°C
Control Inhibitor:
MK 571
Control Activator:
LTD₄
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:
16
Turnaround Time
Standard:
20 Business Days
Reference Compound Data
Clinical Relevance
Therapeutic Area:
Inflammation/Allergy
Additional Information
Brand:
LeadHunter
Testing Location:
Taiwan - Taipei
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