PAR1 Assay(s)

Background Information

Protease-activated receptor 1 (PAR1). Activated by thrombin-mediated proteolysis of the N-terminus. Mediates platelet activation, vascular smooth muscle contraction, and vascular inflammation. Overexpressed in breast cancer, melanoma, and prostate cancer; promotes tumor invasion, angiogenesis, and metastasis via thrombin signaling.

Family: GPCR
Protein Name: PAR1
Gene Name: F2R

Organism: Human
Therapeutic Area: Cardiovascular, Immunology, Oncology

Assay Information

Validated Assay(s): Calcium Assay
Assay type: Cell-based
Method: Fluorescence

Instrumentation: FLIPR
Plate Format: 384-well
Expression: Transient
Cell type: HEK293T

Testing Information

Functional Mode(s): Agonist, Antagonist
Reference compound(s): TFLLR-NH2

TFLLR-NH2 concentration-response curve for the human PAR1 receptor in a Brilliant Calcium fluorescence assay using HEK293T cells.
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