Alendronate sodium hydrate
(Synonyms: 阿仑膦酸钠; Alendronate; MK 217; G-704650 Adronat) 目录号 : GC10348
Alendronate sodium hydrate是含氮双膦酸盐，强力抑制骨吸收，常用于预防和治疗骨质疏松症的研究。
Cas No.:121268-17-5
Sample solution is provided at 25 µL, 10mM.
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Alendronate sodium hydrate is a nitrogen-containing bisphosphonate that strongly inhibits bone resorption, it is often used in research on the prevention and treatment of osteoporosis [1]. Alendronate sodium hydrate has a strong affinity for circulating calcium and minerals on the bone surface, and inhibits the enzyme activity in osteoclasts, thereby hindering the dissolution of bone tissue and the degradation of collagen [2].
Alendronate sodium hydrate (10-4mol/L) incubated for 48 hours significantly reduced the collagen synthesis of osteoblasts. Alendronate sodium hydrate at a concentration of 10-12-10-5mol/L has no effect on calcium deposition in normal human osteoblasts [3].
Alendronate sodium hydrate (25mg/kg) treatment twice each week for 8 weeks, exhibited a reversal of mouse liver fibrosis to a significant extent, and the expression of α-SMA positive cells in the hepatic fibrosis area was significantly reduced in CCl4 induced liver fibrosis mouse model [4]. Alendronate sodium hydrate (0.01 to 0.25mg/kg, s.c., 11 days) preserves alveolar bone resorption and has anti-inflammatory and antibacterial activities in experimental periodontitis [5]. Alendronate sodium hydrate pretreated mice (0.1mg/kg twice a week or once a week) combined with paclitaxel administration (10-50mg/kg/day twice a week or once a week) statistically significantly blocked the growth of PC3 ML tumors in bone marrow and soft tissue. And significantly improve survival time [6].
References:
[1] Bell NH, Johnson RH. Bisphosphonates in the treatment of osteoporosis. Endocrine. 1997 Apr;6:203-6.
[2] Iwamoto J, Miyata A, Sato Y, Takeda T, Matsumoto H. Five-year alendronate treatment outcome in older postmenopausal Japanese women with osteoporosis or osteopenia and clinical risk factors for fractures. Therapeutics and Clinical Risk Management. 2009 Oct 12:773-9.
[3] Garcia-Moreno C, Serrano S, Nacher M, Farré M, Diez A, Marinoso ML, Carbonell J, Mellibovsky L, Nogués X, Ballester J, Aubía J. Effect of alendronate on cultured normal human osteoblasts. Bone. 1998 Mar 1;22(3):233-9.
[4] Bi WR, Jin CX, Xu GT, Yang CQ. Effect of alendronate sodium on the expression of mesenchymal-epithelial transition markers in mice with liver fibrosis. Experimental and Therapeutic Medicine. 2013 Jan;5(1):247-52.
[5] Menezes AM, Rocha FA, Chaves HV, Carvalho CB, Ribeiro RA, Brito GA. Effect of sodium alendronate on alveolar bone resorption in experimental periodontitis in rats. Journal of periodontology. 2005 Nov;76(11):1901-9.
[6] Stearns ME, Wang M. Effects of alendronate and taxol on PC-3 ML cell bone metastases in SCID mice. Invasion & Metastasis. 1996 Jan 1;16(3):116-31.
Alendronate sodium hydrate是含氮双膦酸盐，强力抑制骨吸收，常用于预防和治疗骨质疏松症的研究[1]。Alendronate sodium hydrate 对循环钙和骨表面的矿物质具有很强的亲和力，并抑制破骨细胞中的酶活性，从而阻碍骨组织的溶解和胶原蛋白的降解[2]。
Alendronate sodium hydrate(10-4mol/L)孵育48 h显著减少了成骨细胞的胶原合成。10-12-10-5mol/L浓度的Alendronate sodium hydrate对正常人成骨细胞的钙沉积无影响[3]。
每周两次给予Alendronate sodium hydrate（25mg/kg），持续 8 周，可显著逆转小鼠肝纤维化，CCl4 诱发的肝纤维化小鼠模型中肝纤维化区域 α-SMA 阳性细胞的表达显著降低 [4]。Alendronate sodium hydrate（0.01 to 0.25mg/kg, s.c., 11 days）可保持牙槽骨吸收，并在实验性牙周炎中具有抗炎和抗菌活性[5]。lendronate sodium hydrate预处理小鼠(0.1mg/kg，一周两次或一周一次)，并联合紫杉醇给药(10-50mg/kg/day，一周两次或一周一次)统计学上显著阻断骨髓和软组织中PC-3 ML肿瘤的生长，并显著提高生存时间 [6]。
| Cell experiment [1]: | |
Cell lines | Human bone cells |
Preparation Method | A stock solution of Alendronate sodium hydrate was prepared by dissolving at a concentration of 10mol/L in DMEM. Culture media were prepared at final concentrations of alendronate between 10-12 to 10-1mol/L, with 1:10 serial dilutions of the stock solutions. Medium with or without Alendronate sodium hydrate was then added and the cells incubated for 48 or 96h. |
Reaction Conditions | 10-12 to 10-1mol/L; 48 or 96h |
Applications | After 96 h of incubation, cell viability was significantly decreased at the Alendronate sodium hydrate concentration of 10-4mol/L. |
| Animal experiment [2]: | |
Animal models | Ovariectomized female Wistar rats |
Preparation Method | The animals were divided into four groups: ovariectomized (OVX group); ovariectomized and treated with 1mg/kg or 2mg/kg Alendronate sodium hydrate (ALN) salt diluted in saline solution (Group OVX + ALN1 and Group OVX + ALN2); and a sham operated group used as the control. |
Dosage form | 1 or 2mg/kg; s.c.; twice a week |
Applications | The rats began treatment immediately following ovariectomy and both doses of Alendronate sodium hydrate proved effectiveness in controlling mineral loss. |
References: | |
| Cas No. | 121268-17-5 | SDF | |
| 别名 | 阿仑膦酸钠; Alendronate; MK 217; G-704650 Adronat | ||
| 化学名 | sodium hydrogen(4-amino-1-hydroxy-1-phosphonobutyl)phosphonate trihydrate | ||
| Canonical SMILES | [O-]P(O[H])(C(O[H])(C([H])([H])C([H])([H])C([H])([H])N([H])[H])P(O[H])(O[H])=O)=O.[H]O[H].[H]O[H].[H]O[H].[Na+] | ||
| 分子式 | C4H18NNaO10P2 | 分子量 | 325.12 |
| 溶解度 | ≥ 5.57mg/mL in Water | 储存条件 | Store at -20°C |
| General tips | 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；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.0758 mL | 15.3789 mL | 30.7579 mL |
| 5 mM | 0.6152 mL | 3.0758 mL | 6.1516 mL |
| 10 mM | 0.3076 mL | 1.5379 mL | 3.0758 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet