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]. Animal Model: Ovariectomized 12 weeks old C57Bl6J mice[2] Dosage: 10 mg/kg Administration: i.p.; 5 consecutive days per week; for 6 weeks Result: Corrected ovariectomy-induced osteopenia in mice by inducing new bone formation.
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].
Kinase Assay
Cell Assay
Animal Administration
References
[1]. Hideo Satsu, et al. A sphingosine 1-phosphate receptor 2 selective allosteric agonist. Bioorg Med Chem. 2013 Sep 1;21(17):5373-82.
[2]. Sarah Weske, et al. Agonist-induced activation of the S1P receptor 2 constitutes a novel osteoanabolic therapy for the treatment of osteoporosis in mice. Bone. 2019 Aug;125:1-7.
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