CYM-5520

CYM-5520 is a selective and allosteric sphingosine 1-phosphate receptor 2 (S1PR2) agonist with an EC₅₀ of 480 nM. CYM-5520 does not activate S1PR1, S1PR3, S1PR4 and S1PR5 receptors. CYM-5520 can co-bind in the S1PR2 receptor with S1P. CYM-5520 can be used for osteoporosis research^[1][2]. In Vitro: CYM-5520 (EC₅₀ of 1.6 μM) is a full agonist for wild type S1PR2. Stimulation of cells expressing the triple mutant S1PR2 with S1P does not elicit a rise in luciferase activity, whereas the CYM-5520 is an agonist with an EC₅₀ of 1.5 μM^[1]. In Vivo: CYM-5520 (10 mg/kg; i.p.; 5 consecutive days per week; for 6 weeks) treatment clearly increases long bone and vertebral bone mass in osteopenic ovariectomized mice. CYM-5520 also increases osteoblast number, osteoid surface and alkaline phosphatase, and plasma concentrations of the osteoanabolic marker procollagen I C-terminal propeptide are also elevated^[2].