Zoledronic Acid

国际站：Zoledronic Acid

中文名：唑来膦酸

CAS：118072-93-8

品牌：MedChemExpress (MCE)

存储条件：Please store the product under the recommended conditions in the Certificate of Analysis.

生物活性：Zoledronic Acid (Zoledronate) 是第三代双膦酸盐 (BP)，具有强大的抗再吸收活性。 Zoledronic Acid 抑制破骨细胞的分化和凋亡。唑来膦酸还具有抗癌作用。

体外：Zoledronic Acid（0.1-1 µM；48 小时）增加骨细胞样 MLO-Y4 细胞中核因子 kB 配体 (RANKL) 和硬化蛋白 mRNA 表达的受体激活剂^[2]。Zoledronic酸增加MLO-Y4细胞破骨细胞生成支持因子的表达^[2]。唑来膦酸通过IL-6/JAK2/STAT3通路增强MLO-Y4细胞中RANKL的表达^[2].唑来膦酸通过调控NF-κB和JNK信号通路抑制破骨细胞分化和功能^[3].唑来膦酸(10 -100 µM；1-7 天）显着降低 MC3T3-E1 细胞的活力^[4]。唑来膦酸（10-100 µM；1-7 天）诱导 MC3T3 细胞凋亡-E1 细胞^[4]。Zoledronic Acid（10-100 µM；4 天）因诱导细胞凋亡而抑制细胞活力^[4]。< br/> 唑来膦酸在浓度 <1 µM^[4].

体内：唑来膦酸（0.05 毫克/千克；腹腔注射；每周；持续 3 周）增加骨矿物质密度和含量^[5]。唑来膦酸（0.5-1 毫克/千克；腹腔注射；每周; 持续 3 周）抑制破骨细胞和成骨细胞的功能以及体内骨重塑，干扰骨力学性能^[5]。

参考文献：[1]. Lianwei Wang, et al. Various pathways of zoledronic acid against osteoclasts and bone cancer metastasis: a brief review. BMC Cancer. 2020; 20: 1059.[2]. Hyung Joon Kim, et al. Zoledronate Enhances Osteocyte-Mediated Osteoclast Differentiation by IL-6/RANKL Axis. Int J Mol Sci. 2019 Mar; 20(6): 1467.[3]. Xiao-Lin Huang, et al. Zoledronic acid inhibits osteoclast differentiation and function through the regulation of NF-κB and JNK signalling pathways. Int J Mol Med. 2019 Aug;44(2):582-592.[4]. XIN HUANG, et al. Dose-dependent inhibitory effects of zoledronic acid on osteoblast viability and function in vitro. Mol Med Rep. 2016 Jan; 13(1): 613-622.[5]. Samantha Pozzi, et al. High-dose zoledronic acid impacts bone remodeling with effects on osteoblastic lineage and bone mechanical properties. Clin Cancer Res. 2009 Sep 15;15(18):5829-39.[6]. Shea GKH, et al. Oral Zoledronic acid bisphosphonate for the treatment of chronic low back pain with associated Modic changes: A pilot randomized controlled trial. J Orthop Res. 2022 Feb 23.