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. Author manuscript; available in PMC: 2012 Jan 1.
Published in final edited form as: Trends Pharmacol Sci. 2010 Dec 14;32(1):16–24. doi: 10.1016/j.tips.2010.11.002

Table 1. Major compounds that target S1P and S1P receptors.

Compound Target specificity Status of clinical and preclinical development
FTY720 Agonist/functional antagonist for S1P1, S1P3, S1P4, S1P5 Approved by FDA for multiple sclerosis treatment (2010)
KRP-203 Agonist for S1P1 Phase I clinical trials for multiple sclerosis
SEW2871 Agonist for S1P1 Animal models of renal ischemia-reperfusion injury
W146 Antagonist for S1P1 N/A
VPC23019 Antagonist for S1P1, S1P3 N/A
JTE-013 Antagonist for S1P2 N/A
DMS Inhibitor for SphKs Animal inflammatory models such as asthma and arthritis
SKI-II Inhibitor for SphKs Animal tumor models
SK1-I Inhibitor for SphK1 Animal tumor models
5c Inhibitor for SphK1 Animal models of bacterial sepsis
ABC294640 Inhibitor for SphK2 Animal tumor models
LT1009 Humanized antibody for S1P Phase I clinical trials for cancer and macular degeneration
LX2931 Inhibitor for S1P lyase Phase II clinical trials for rheumatoid arthritis