Strontium Ranelate (S12911) 是一种抗骨质疏松药物,其作用是通过减少骨吸收并促进骨形成,从而诱导正骨平衡。Strontium Ranelate 还可以激活非骨骼细胞中的钙敏感受体 (CaSR),从而导致肌醇 1、4、5-三磷酸生成和丝裂原活化的蛋白激酶信号转导。
生物活性 | Strontium Ranelate (S12911) is an antiosteoporotic agent that acts by reducing bone resorption and promoting bone formation, thereby inducing a positive bone balance. Strontium Ranelate can also activate thecalcium-sensing receptor (CaSR)in non skeletal cells, resulting in the activation of inositol 1, 4, 5-triphosphate production andmitogen-activated protein kinasesignaling[1][2]. |
体外研究 (In Vitro) | Strontium Ranelate (0.1-1 mM; 22 days; Mouse calvaria cells) treatment shows the expression of mRNA for early osteoblast markers (alkaline phosphatase, ALP) is visualized by day 5, while late markers (osteocalcin, OCN) are detectable only by day 15 and beyond[1]. Strontium Ranelate (0.1-1 mM; 22 days; Mouse calvaria cells) treatment results in significantly increases the mRNA expression of the osteoblastic markers ALP, BSP and OCN at day 22 of MC cell culture[1]. Strontium Ranelate is found to increase alkaline phosphatase activity and prostaglandin E2 production in a COX-2 dependent manner in murine marrow stromal cells[2].
RT-PCR[1] Cell Line: | Mouse calvaria (MC) cells | Concentration: | 0.1 mM, 0.3 mM or 1 mM | Incubation Time: | 22 days | Result: | The expression of mRNA for early osteoblast markers (ALP) was visualized by day 5, while late markers (OCN) were detectable only by day 15 and beyond. |
Western Blot Analysis[1] Cell Line: | Mouse calvaria (MC) cells | Concentration: | 0.1 mM, 0.3 mM or 1 mM | Incubation Time: | 22 days | Result: | Significantly increased the mRNA expression of the osteoblastic markers ALP, BSP and OCN at day 22 of MC cell culture. |
|
体内研究 (In Vivo) | Strontium Ranelate increases bone formation and decreased bone resorption, which results in increased bone mass in the vertebrae of intact adult mice[2]. In intact adult rats, Strontium Ranelate also increases bone mass, as measured by dual-energy X-ray absorptiometry, in lumbar vertebra and femur, and this is confirmed by histological assessment of trabecular bone volume in the tibial metaphysis[2]. Strontium Ranelate is found to decrease bone resorption and to increase bone formation in alveolar bone in normal adult monkeys (Macaca fascicularis), which exhibits extensive bone remodeling[2]. In ovariectomized rats, short-term (3 months) treatment with Strontium Ranelate prevents trabecular bone loss induced by oestrogen deficiency, as demonstrated by bone ash, bone mineral content and histomorphometric analysis in the tibial metaphysis. This effect results from decreased bone resorption while bone formation was maintained. These beneficial effects of Strontium Ranelate on bone mass and microarchitecture in ovariectomized rats are confirmed in long-term experiments. In this long-term study (2 years), the increase in bone mass and microarchitecture induced by Strontium Ranelate results in a marked improvement in bone strength, supporting the beneficial effect of this drug on bone resistance[2].
|
Clinical Trial | |
分子量 | |
性状 | |
Formula | |
CAS 号 | |
中文名称 | |
运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | 4°C, sealed storage, away from moisture *该产品在溶液状态不稳定,建议您现用现配,即刻使用。 |
溶解性数据 | In Vitro: 0.1 M HCL : 17.5 mg/mL(34.08 mM;ultrasonic and adjust pH to 3 with HCl) H2O : 2 mg/mL(3.89 mM;ultrasonic and warming and heat to 60℃) DMSO :< 1 mg/mL(insoluble or slightly soluble) 配制储备液 1 mM | 1.9475 mL | 9.7373 mL | 19.4746 mL | 5 mM | 0.3895 mL | 1.9475 mL | 3.8949 mL | 10 mM | 0.1947 mL | 0.9737 mL | 1.9475 mL |
*请根据产品在不同溶剂中的溶解度,选择合适的溶剂配制储备液;该产品在溶液状态不稳定,建议您现用现配,即刻使用。 |