Pamidronate
(Synonyms: 帕米膦酸) 目录号 : GC11115
An FPP synthase inhibitor that inhibits bone resorption
Cas No.:40391-99-9
Sample solution is provided at 25 µL, 10mM.
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Pamidronic acid is a drug used to treat a broad spectrum of bone absorption diseases.
Osteosarcoma cell viability decreases significantly in a concentration- and time-dependent manner at pamidronate concentrations ranging from 100 to 1000 μM, most consistently after 48 and 72 hours' exposure. In treated osteosarcoma cells, the lowest percentage cell viability is 34% (detected after 72 hours' exposure to 1000μM pamidronate)[1]. Pamidronate disodium inhibits Wnt and β-catenin signaling, which controls osteogenic differentiation in BMMSCs. Wnt3a, a Wnt and β-catenin signaling activator, reverses the negative effects caused by pamidronate disodium to salvage the osteogenic defect in BMMSCs[2].
Pamidronic acid can significantly inhibit and even reverse early osteoarthritic subchondral bone loss, thus alleviating the process of cartilaginous degeneration. The mechanisms involved may be associated with the upregulation of OPG expression, and downregulation of RANKL, MMP-9 and TLR-4 expression[3].
Reference:
[1]. Ashton JA, et al. Investigation of the effect of pamidronate disodium on the in vitro viability of osteosarcoma cellsfrom dogs. Am J Vet Res. 2005 May;66(5):885-91.
[2]. Xu Y, et al. Pamidronate Disodium Leads to Bone Necrosis via Suppression of Wnt/β-Catenin Signaling in Human Bone Marrow Mesenchymal Stem Cells In Vitro. J Oral Maxillofac Surg. 2017 Mar 22.
[3]. Lv Y, et al. Effects of pamidronate disodium on the loss of osteoarthritic subchondral bone and the expression of cartilaginous and subchondral osteoprotegerin and RANKL in rabbits. BMC Musculoskelet Disord. 2014 Nov 6;15:370.
Cell experiment: | Cell counts and cell viability assays are performed in cultures of osteosarcoma cells (POS, HMPOS, and COS31 cell lines) and fibroblasts after 24, 48, and 72 hours of incubation with pamidronate at concentrations of 0.001 to 1000 microM or with no drug (control treatment). Percentage viability is determined in cell samples for each concentration of pamidronate and each incubation time. A DNA fragmentation analysis is performed to assess bisphosphonate-induced apoptosis[1]. |
Animal experiment: | Rabbits: The rabbits are randomly divided into four groups. Sham-operated with vehicle treatment, OA induced by ACLT with vehicle treatment, OA-induced ACLT treated with short-term pamidronic acid treatment after ACLT, and ACLT treated with long-term PAM treatment. PAM is injected at the 4th week after ACLT in PAM-S and PAM-L groups, and followed by once monthly ear vein injections at a dosage of 3 mg/kg body weight. In the other groups, only saline infusions of equal volumes are administered. 10 animals are humanely sacrificed at both 2 and 10 weeks after pamidronic acid treatment. In the ACLT and Sham groups, five animals are sacrificed at 2, 4, 6, and 14 weeks after model establishment[3]. |
References: [1]. Ashton JA, et al. Investigation of the effect of pamidronate disodium on the in vitro viability of osteosarcoma cellsfrom dogs. Am J Vet Res. 2005 May;66(5):885-91. | |
| Cas No. | 40391-99-9 | SDF | |
| 别名 | 帕米膦酸 | ||
| 化学名 | (3-amino-1-hydroxy-1-phosphonopropyl)phosphonic acid | ||
| Canonical SMILES | C(CN)C(O)(P(=O)(O)O)P(=O)(O)O | ||
| 分子式 | C3H11NO7P2 | 分子量 | 235.07 |
| 溶解度 | ≥ 2.35mg/mL in Water with gentle warming, <2.35mg/mL in DMSO | 储存条件 | -20°C, protect from light |
| 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 | 4.2541 mL | 21.2703 mL | 42.5405 mL |
| 5 mM | 0.8508 mL | 4.2541 mL | 8.5081 mL |
| 10 mM | 0.4254 mL | 2.127 mL | 4.2541 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。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet