WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H200133
CAS#: 121268-17-5 (sodium hydrate)
Description: Alendronate sodium is the sodium salt of alendronate, a second generation bisphosphonate and synthetic analog of pyrophosphate with bone anti-resorption activity. Alendronate sodium binds to and inhibits the activity of geranyltranstransferase (farnesyl pyrophosphate synthetase), an enzyme involved in terpenoid biosynthesis. Inhibition of this enzyme prevents the biosynthesis of isoprenoid lipids (FPP and GGPP) that are donor substrates of farnesylation and geranylgeranylation during the post-translational modification of small GTPase signalling proteins, which is important in the process of osteoclast turnover.
Hodoodo Cat#: H200133
Name: Alendronate sodium
CAS#: 121268-17-5 (sodium hydrate)
Chemical Formula: C4H18NNaO10P2
Exact Mass: 0.00
Molecular Weight: 325.120
Elemental Analysis: C, 14.78; H, 5.58; N, 4.31; Na, 7.07; O, 49.21; P, 19.05
Related CAS #: 121268-17-5 (sodium hydrate) 129318-43-0 (sodium) 134606-40-9 (disodium) 66376-36-1 (free acid) 137504-90-6 (calcium) 138624-11-0 (free acid hydrate)
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
More Info:
| 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 |
| 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 | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| Water | 28.6 | 87.88 |
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.
