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Description

Lysophosphatidic acid (LPA) is a lysophospholipid produced by activated platelets that inhibits adenylate cyclase and stimulates DNA synthesis, changes in cell morphology, and increases in intracellular calcium in a variety of cultured mammalian cells. A family of three GPCRs, LPA1, LPA2 and LPA3, mediates the biological effects of LPA (Contos et al., 2000). LPA1 is widely expressed, with particularly notable expression in the ventricular zone of the embryonic cerebral cortex. Mice lacking LPA1 exhibit craniofacial abnormalities and defective development of the cerebral cortex (Harrison et al., 2003, Choi et al., 2008). LPA1 also promotes fibrotic responses to tissue injury (Tager et al., 2008) Millipore's LPA1 Membrane Preparation is a crude membrane preparation made from the proprietary stable recombinant cell line that is also used for Millipore's LPA1 Calcium Optimized Cell Line (HTS089C). This LPA1 Membrane Preparation exhibits both constitutive and agonist-induced activity in GTPgammaS binding assays, thus it is an ideal HTS tool for screening of compounds for agonist, inverse agonist, and antagonist activities. The membrane preparations exhibits EC50 of 73 nM for LPA in a GTPgammaS binding assay., Human EDG2 encoding LPA1