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Chemical Compound Review:

AC1NSKEE [2-[[(Z)-octadec-9- enoyl]amino]-3-(4...

Synonyms: CHEMBL262906, CHEBI:249898, VPC12249

Heasley, B.H. et al., Heise, C.E. et al.

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High impact information on VPC12249

One compound with a bulky hydrophobic group (VPC12249) was a dual LPA1/LPA3 competitive antagonist [1].
A recently reported dual LPA1/LPA3 receptor antagonist (VPC12249, 1) has been modified herein so as to optimize potency and selectivity at LPA receptors [2].

References

Activity of 2-substituted lysophosphatidic acid (LPA) analogs at LPA receptors: discovery of a LPA1/LPA3 receptor antagonist. Heise, C.E., Santos, W.L., Schreihofer, A.M., Heasley, B.H., Mukhin, Y.V., Macdonald, T.L., Lynch, K.R. Mol. Pharmacol. (2001) [Pubmed]
Initial structure-activity relationships of lysophosphatidic acid receptor antagonists: discovery of a high-affinity LPA1/LPA3 receptor antagonist. Heasley, B.H., Jarosz, R., Lynch, K.R., Macdonald, T.L. Bioorg. Med. Chem. Lett. (2004) [Pubmed]

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