The sphingosine 1-phosphate (S1P) receptor S1P₃ has roles in vasodilation, epithelial barrier function, cardioprotection, fibrosis, immunity, and inflammation.^1,2 CYM 5541 is a selective, allosteric agonist of S1P₃ (EC₅₀ = 72-132 nM).^3,4 It less effectively activates S1P₁ (EC₅₀ = 28-38 µM) and is ineffective at S1P₂, S1P₄, and S1P₅ as well as a panel of other receptors, ion channels and transporters.³

≥98%

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1.Choi, J.W.,Lee, C.W. and Chun, J. Biological roles of lysophospholipid receptors revealed by genetic null mice: An update. Biochimica et Biophysica Acta 1781, 531-539 (2008).

2.Rosen, H.,Stevens, R.C.,Hanson, M., et al. Sphingosine-1-phosphate and its receptors: Structure, signaling, and influence. Annual Reviews of Biochemistry 82, 637-662 (2013).

3.Guerrero, M.,Poddutoori, R.,Pinacho-Crisostomo, F., et al. Probe development efforts for an allosteric agonist of the sphingosine 1-phosphate receptor 3 (S1P₃). 1-13 (2011).

4.Jo, E.,Bhhatarai, B.,Repetto, E., et al. Novel selective allosteric and bitopic ligands for the S1P₃ receptor. ACS Chemical Biology 7(12), 1975-1983 (2012).