HUMAN RECOMBINANT P2Y1 RECEPTOR
MULTISCREEN™ STABLE CELL LINES
1 vial (2 x 106) frozen cells
Sigma Freezing Medium (C-6164)
Full-length human P2Y1 cDNA (GenBank Accession Number NM_002563)
Liquid nitrogen upon receiving
Propagation Medium: DMEM, 10% FBS, 100 µg/mL G418
Stable after minimum of two months continuous growth
Background: P2Y1 is a receptor for ATP and ADP. P2Y1 contributes to platelet shape change. A number of P2Y1 receptor-specific antagonists, such as, MRS-2179, A3P5PS, A3P5P and A2P5P have been discovered. They inhibit calcium ion mobilization and shape change in platelets. P2Y1-deficient mice and mice treated with the P2Y1 antagonist MRS2179 displayed significantly less arterial thrombosis than their respective controls. Combination of P2Y1 deficiency with P2Y12 inhibition led to a significant additive effect.
Application: Functional assays
Figure legend: Dose-dependent stimulation of calcium flux upon treatment with ligand, measured with MultiscreenTM Calcium 1.0 No Wash Assay Kit (Multispan MSCA01).
Baurand and Gachet (2003) The P2Y(1) receptor as a target for new antithrombotic drugs: a review of the P2Y(1) antagonist MRS-2179. Cardiovasc Drug Rev 21:67-76.
Jin et al. (1998) Molecular basis for ADP-induced platelet activation. II. The P2Y1 receptor mediates ADP-induced intracellular calcium mobilization and shape change in platelets. J Biol Chem 273:2030-2034.
Lenain et al. (2003) Inhibition of localized thrombosis in P2Y1-deficient mice and rodents treated with MRS2179, a P2Y1 receptor antagonist. J Thromb Haemost 1:1144-1149.