Sphingosine 1-phosphate (S1P) is a well-defined bioactive lipid molecule derived from membrane sphingolipid metabolism. In the past decades, a series of key enzymes involved in generation of S1P have been identified and characterized in detail, as well as enzymes degrading S1P. S1P requires transporter to cross the plasma membrane and carrier to deliver to its cognate receptors and therefore transduces signaling in autocrine, paracrine, or endocrine fashions. The essential roles in regulation of development, metabolism, inflammation, and many other aspects of life are mainly executed when S1P binds to receptors provoking the downstream signaling cascades in distinct cells. This chapter will review the synthesis, degradation, transportation, and signaling of S1P and try to provide a comprehensive view of the biology of S1P, evoking new enthusiasms and ideas into the field of the fascinating S1P.