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编 号:F167003
分子式:C21H19N3O2
分子量:345.39
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10mM*1mL in DMSO
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1mg
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5mg
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10mg
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25mg
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50mg
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100mg
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生物活性:
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.

体内研究:
CYM-5520 (10 mg/kg;腹腔注射;每周连续 5 天;持续 6 周) 处理明显增加骨质减少的卵巢切除小鼠的长骨和椎骨骨量。CYM-5520 还增加成骨细胞数量、类骨质表面和碱性磷酸酶,骨合成代谢标志物前胶原 I C 端前肽的血浆浓度也升高。Animal Model:Ovariectomized 12 weeks old C57Bl6J mice
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.

体外研究:
CYM-5520 (EC50 为 1.6 μM) 是野生型 S1PR2 的完全激动剂。用 S1P 刺激表达三重突变体 S1PR2 的细胞不会引起荧光素酶活性的升高,而 CYM-5520 是一种激动剂,EC50 为 1.5 μM。
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