Synonym
Alendronate sodium; Alendronate disodium; Fosamax: Adronat; Alendros; Onclast. Code names: G704650; G-704650; G 704650; MK217; MK-217; MK 217;
IUPAC/Chemical Name
(4-amino-1-hydroxybutylidene) bisphosphonic acid monosodium salt trihydrate.
InChi Key
DCSBSVSZJRSITC-UHFFFAOYSA-M
InChi Code
InChI=1S/C4H13NO7P2.Na.3H2O/c5-3-1-2-4(6,13(7,8)9)14(10,11)12;;;;/h6H,1-3,5H2,(H2,7,8,9)(H2,10,11,12);;3*1H2/q;+1;;;/p-1
SMILES Code
OC(P([O-])(O)=O)(P(O)(O)=O)CCCN.[H]O[H].[H]O[H].[H]O[H].[Na+]
Appearance
white solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in water
Shelf Life
>10 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
Biological target:
Alendronate (sodium hydrate) is a farnesyl diphosphate synthase inhibitor with IC50 of 460 nM.
In vitro activity:
Cultures treated with the highest alendronate concentration (100 μM Ald) showed significantly lower percentages of live cells than the other groups (control, 0.1, 1 and 10 μM Ald) after 24 h (p < 0.001). The rate of live cells in the 100 μM Ald group significantly decreased with time dependence (p < 0.001), reaching 24.53 ± 7.71% (mean ± SD) of total cells in 5 days. The rates of live cells in control, 0.1, 1 and 10 μM Ald did not differ significantly from one another (p > 0.05) (Fig. 2a). According to the morphological analyses using phase contrast microscope and crystal violet staining, the cell population was markedly more decreased in the 100 μM Ald group than in the other studied groups (Fig. 2b and c).
Reference: BMC Musculoskelet Disord. 2020; 21: 19. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6955091/
In vivo activity:
The results in Fig. 5A revealed that bone structure was significantly improved in rats treated with alendronate that exhibited ovariectomy-induced osteoporosis compared with the PBS group. It was also observed that alendronate treatment prevented loss of trabeculae in rats with osteoporosis induced by ovariectomy (Fig. 5B). In addition, bone strength and bone density assays demonstrated that alendronate significantly improved osteoporosis in rats induced by ovariectomy, when compared with the PBS control group (Fig. 5C and D). Furthermore, the elastic modulus and post-yield displacement of bone were also increased in rats with osteoporosis following treatment with alendronate (Fig. 5E and F). Therefore, these data suggest that alendronate treatment was beneficial in rats with osteoporosis induced by ovariectomy, as determined by histological and index detection.
Reference: Exp Ther Med. 2018 Jan; 15(1): 182–190. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5763659/
|
Solvent |
mg/mL |
mM |
| Solubility |
| Water |
28.6 |
87.88 |
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.
Preparing Stock Solutions
The following data is based on the
product
molecular weight
325.12
Batch specific molecular weights may vary
from batch to batch
due to the degree of hydration, which will
affect the solvent
volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass |
1 mg |
5 mg |
10 mg |
| 1 mM |
1.15 mL |
5.76 mL |
11.51 mL |
| 5 mM |
0.23 mL |
1.15 mL |
2.3 mL |
| 10 mM |
0.12 mL |
0.58 mL |
1.15 mL |
| 50 mM |
0.02 mL |
0.12 mL |
0.23 mL |
Formulation protocol:
1. Sung CM, Kim RJ, Hah YS, Gwark JY, Park HB. In vitro effects of alendronate on fibroblasts of the human rotator cuff tendon. BMC Musculoskelet Disord. 2020 Jan 11;21(1):19. doi: 10.1186/s12891-019-3014-1. PMID: 31926548; PMCID: PMC6955091.
2. Pourgonabadi S, Ghorbani A, Tayarani Najarn Z, Mousavi SH. In vitro assessment of alendronate toxic and apoptotic effects on human dental pulp stem cells. Iran J Basic Med Sci. 2018 Sep;21(9):905-910. doi: 10.22038/IJBMS.2018.22877.5816. PMID: 30524690; PMCID: PMC6272077.
3. Ma X, Xu Z, Ding S, Yi G, Wang Q. Alendronate promotes osteoblast differentiation and bone formation in ovariectomy-induced osteoporosis through interferon-β/signal transducer and activator of transcription 1 pathway. Exp Ther Med. 2018 Jan;15(1):182-190. doi: 10.3892/etm.2017.5381. Epub 2017 Oct 27. PMID: 29375681; PMCID: PMC5763659.
4. Chuguransky SR, Cortizo AM, McCarthy AD. Alendronate Can Improve Bone Alterations in Experimental Diabetes by Preventing Antiosteogenic, Antichondrogenic, and Proadipocytic Effects of AGEs on Bone Marrow Progenitor Cells. Biomed Res Int. 2016;2016:5891925. doi: 10.1155/2016/5891925. Epub 2016 Oct 20. PMID: 27840829; PMCID: PMC5093246.
In vitro protocol:
1. Sung CM, Kim RJ, Hah YS, Gwark JY, Park HB. In vitro effects of alendronate on fibroblasts of the human rotator cuff tendon. BMC Musculoskelet Disord. 2020 Jan 11;21(1):19. doi: 10.1186/s12891-019-3014-1. PMID: 31926548; PMCID: PMC6955091.
2. Pourgonabadi S, Ghorbani A, Tayarani Najarn Z, Mousavi SH. In vitro assessment of alendronate toxic and apoptotic effects on human dental pulp stem cells. Iran J Basic Med Sci. 2018 Sep;21(9):905-910. doi: 10.22038/IJBMS.2018.22877.5816. PMID: 30524690; PMCID: PMC6272077.
In vivo protocol:
1. Ma X, Xu Z, Ding S, Yi G, Wang Q. Alendronate promotes osteoblast differentiation and bone formation in ovariectomy-induced osteoporosis through interferon-β/signal transducer and activator of transcription 1 pathway. Exp Ther Med. 2018 Jan;15(1):182-190. doi: 10.3892/etm.2017.5381. Epub 2017 Oct 27. PMID: 29375681; PMCID: PMC5763659.
2. Chuguransky SR, Cortizo AM, McCarthy AD. Alendronate Can Improve Bone Alterations in Experimental Diabetes by Preventing Antiosteogenic, Antichondrogenic, and Proadipocytic Effects of AGEs on Bone Marrow Progenitor Cells. Biomed Res Int. 2016;2016:5891925. doi: 10.1155/2016/5891925. Epub 2016 Oct 20. PMID: 27840829; PMCID: PMC5093246.
1: Imai K. Alendronate sodium hydrate (oral jelly) for the treatment of osteoporosis: review of a novel, easy to swallow formulation. Clin Interv Aging. 2013;8:681-8. doi: 10.2147/CIA.S37199. Epub 2013 Jun 7. Review. PubMed PMID: 23766643; PubMed Central PMCID: PMC3679967.
2: Ananchenko G, Novakovic J, Tikhomirova A. Alendronate sodium. Profiles Drug Subst Excip Relat Methodol. 2013;38:1-33. doi: 10.1016/B978-0-12-407691-4.00001-0. Review. PubMed PMID: 23668401.
3: Von Schacht E, Dambacher MA, Ringe JD, Dukas L. [Combination of alendronate plus alfacalcidol in the treatment of osteoporosis. Rationale, preclinical data and clinical evidence]. MMW Fortschr Med. 2012 Apr 5;154 Suppl 1:10-21. Review. German. PubMed PMID: 23427364.
4: Hanna J, Bee J, Sataloff RT. Laryngeal ulceration and hemoptysis secondary to inadvertent alendronate overdose: case report and review of the literature. Ear Nose Throat J. 2012 Nov;91(11):484-5. Review. PubMed PMID: 23288794.
5: He D, Yin M, Luo Y, Wei Q. [Research progress of protective effects of alendronate on articular cartilage in osteoarthritis]. Zhongguo Xiu Fu Chong Jian Wai Ke Za Zhi. 2012 Oct;26(10):1187-90. Review. Chinese. PubMed PMID: 23167100.
6: Emad Y, Ragab Y, El-Shaarawy N, Rasker JJ. Transient osteoporosis of the hip, complete resolution after treatment with alendronate as observed by MRI description of eight cases and review of the literature. Clin Rheumatol. 2012 Nov;31(11):1641-7. doi: 10.1007/s10067-012-2060-y. Epub 2012 Aug 30. Review. PubMed PMID: 22933125.
7: Lin T, Wang C, Cai XZ, Zhao X, Shi MM, Ying ZM, Yuan FZ, Guo C, Yan SG. Comparison of clinical efficacy and safety between denosumab and alendronate in postmenopausal women with osteoporosis: a meta-analysis. Int J Clin Pract. 2012 Apr;66(4):399-408. doi: 10.1111/j.1742-1241.2011.02806.x. Epub 2012 Feb 7. Review. PubMed PMID: 22313934.
8: Gutman D, Golomb G. Liposomal alendronate for the treatment of restenosis. J Control Release. 2012 Jul 20;161(2):619-27. doi: 10.1016/j.jconrel.2011.11.037. Epub 2011 Dec 8. Review. PubMed PMID: 22178594.
9: Kharazmi M, Sjöqvist K, Warfvinge G. Oral ulcers, a little known adverse effect of alendronate: review of the literature. J Oral Maxillofac Surg. 2012 Apr;70(4):830-6. doi: 10.1016/j.joms.2011.03.046. Epub 2011 Aug 4. Review. PubMed PMID: 21816532.
10: Imai K. Vertebral fracture risk and alendronate effects on osteoporosis assessed by a computed tomography-based nonlinear finite element method. J Bone Miner Metab. 2011 Nov;29(6):645-51. doi: 10.1007/s00774-011-0281-9. Epub 2011 Jun 14. Review. PubMed PMID: 21667358.
