139262-76-3

H2L5186303 (139262-76-3) is a potent and selective lysophosphatidic acid 2 (LPA2) receptor antagonist.? IC50?= 8.9 nM, 1230 nM and 27.35 μM for LPA2, LPA3, and LPA1 respectively.1,2

H2L5186303 is an antidepressant acting on the LPA1 (lysophosphatidic acid receptor 1) and induce insulin-like growth factor-I receptor transactivation as well as causing enhanced cell proliferation.

H2L5186303 is specific antagonist of the lysophosphatidic acid receptor LPA2 (Ki = 7.2 nM). The compound H2L5186303 displays 40- to 1800-fold selectivity over other LPA receptors.

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1) Fells?et al. (2008)?Identification of non-lipid LPA3 antagonists by virtual screening; Bioorg. Med. Chem.?16?6207 2) Fells?et al. (2009)?Structure-based drug design identifies novel LPA3 antagonists; Bioorg. Med. Chem. 17?7457