Description
OMPT is a selective agonist of the LPA3 receptor. It exhibits EC50 values of 68 nM and >6.8 µM for calcium mobilization in LPA3 and LPA2-expressing Sf9 cells, respectively.1 The (2S)-OMPT enantiomer is 5- to 20-fold more active than (2R)-OMPT in calcium release assays in both LPA3-transfected Sf9 and rat hepatoma Rh7777 cells.2
1. Hasegawa, Y., Erickson, J.R., Goddard, G.J., Yu, S., Liu, S., Cheng, K.W., Eder, A., Bandoh, K., Aoki, J., Jarosz, R., Schrier, A.D., Lynch, K.R., Mills, G.B., Fang, X. (2003) Identification of a phosphothionate analogue of lysophosphatidic acid (LPA) as a selective agonist of the LPA3 receptor. J Biol Chem 278:11962-11969.
2. Qian, L., Xu, Y., Hasegawa, Y., Aoki, J., Mills, G.B., Prestwich, G.D. (2003) Enantioselective responses to a phosphorothioate analogue of lysophosphatidic acid with LPA3 receptor-selective agonist activity. J Med Chem 46:5575-5578.
References
Hasegawa, Y., Erickson, J.R., Goddard, G.J., Yu, S., Liu, S., Cheng, K.W., Eder, A., Bandoh, K., Aoki, J., Jarosz, R., Schrier, A.D., Lynch, K.R., Mills, G.B., Fang, X. (2003) Identification of a phosphothionate analogue of lysophosphatidic acid (LPA) as a selective agonist of the LPA3 receptor. J Biol Chem 278:11962-11969.
Qian, L., Xu, Y., Hasegawa, Y., Aoki, J., Mills, G.B., Prestwich, G.D. (2003) Enantioselective responses to a phosphorothioate analogue of lysophosphatidic acid with LPA3 receptor-selective agonist activity. J Med Chem 46:5575-5578.