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Chemical Structure| 121268-17-5 Chemical Structure| 121268-17-5

Structure of Alendronate sodium hydrate
CAS No.: 121268-17-5

Chemical Structure| 121268-17-5

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Alendronate Sodium Trihydrate is an inhibitor of farnesyl diphosphate synthase with IC50 of 460 nM. It is used to treat osteoporosis.

Synonyms: Alendronate; MK 217; Fosamax

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Product Details of Alendronate sodium hydrate

CAS No. :121268-17-5
Formula : C4H18NNaO10P2
M.W : 325.12
SMILES Code : OC(P(O)(O)=O)(CCCN)P([O-])(O)=O.[H]O[H].[H]O[H].[H]O[H].[Na+]
Synonyms :
Alendronate; MK 217; Fosamax
MDL No. :MFCD01748233
InChI Key :DCSBSVSZJRSITC-UHFFFAOYSA-M
Pubchem ID :23681107

Safety of Alendronate sodium hydrate

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302
Precautionary Statements:P280-P305+P351+P338

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
Primary human skeletal muscle-derived progenitor cells (HSMPCs) 0.1-1μM 24 h Alendronate significantly reversed dexamethasone-induced myotube atrophy and myogenic differentiation inhibition, and functioned through down-regulation of SIRT3 protein expression J Cachexia Sarcopenia Muscle. 2018 Jun;9(3):585-602
C2C12 mouse myoblasts 0.1-1μM 24 h Alendronate dose-dependently promoted the enlargement in diameters of myotubes and significantly inhibited dexamethasone-induced myotube atrophy and myogenic differentiation inhibition J Cachexia Sarcopenia Muscle. 2018 Jun;9(3):585-602
SKOV3-luc cells 100 mg/L 24 h To evaluate the cytotoxicity of CaALN-N on SKOV3-luc cells, results showed CaALN-N induced apoptosis via down-regulation of HER2 signaling pathway. Adv Sci (Weinh). 2023 May;10(14):e2204654
Bone marrow osteoblastic cells 10 nM or 1 μM 21 days Alendronate inhibited osteoblast differentiation, especially BSP gene expression J Dent Res. 2012 Mar;91(3):268-74

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
ICR mice Denervation-induced muscle atrophy and glycerol-induced muscle injury models Oral administration 0.5 and 1 mg/kg Continuous administration for 1 month until sacrifice at 7 days post-denervation or 5 days post-muscle injury Low-dose alendronate by oral administration ameliorated muscular malfunction and morphological changes in mouse models of denervation-induced muscle atrophy and glycerol-induced muscle injury, functioning through negative regulation of SIRT3 expression J Cachexia Sarcopenia Muscle. 2018 Jun;9(3):585-602
C57Bl/6 mice Osteoporosis model Subcutaneous injection 10 μg/100g/week Once a week for 8 weeks Alendronate indirectly inhibited osteoblast function through pre-osteoclasts, reducing bone formation J Dent Res. 2012 Mar;91(3):268-74
Sprague-Dawley (SD) rats Liquid nitrogen-treated femoral head necrosis model Not specified 100 μM 10 days Alendronate partially reversed the suppression of expression of BMP2, EIF2AK3, EIF2A, ATF4 caused by liquid nitrogen, potentially treating ONFH via targeting the BMP2/EIF2AK3/EIF2A/ATF4 pathway Drug Des Devel Ther. 2021 Apr 23;15:1717-1724

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT00259857 Osteoporosis PHASE2 COMPLETED 2025-08-09 Medical University of South Ca... More >>rolina, Charleston, South Carolina, 29425, United States Less <<
NCT00120757 Osteoporosis|HIV Infections PHASE3 COMPLETED 2025-11-08 Service de Medecine Interne ho... More >>pital Avicenne, Bobigny, 93009 cedex, France|Service de Rhumatologie hopital Pitie-Salpetriere, Paris, 75013, France|H?pital Necker service des Maladies Infectieuses, Paris, 75015, France Less <<
NCT00010439 Osteoporosis PHASE2 COMPLETED 2025-11-08 Medical University of South Ca... More >>rolina, Charleston, South Carolina, 29425, United States Less <<
NCT05091099 Osteoporosis PHASE4 RECRUITING 2025-12-31 National Taiwan University Hos... More >>pital, Yunlin branch, Douliu, Yunlin County, 640, Taiwan Less <<
NCT00277251 Glucocorticoid-Associated Oste... More >>openia and Osteoporosis Less << PHASE2|PHASE3 COMPLETED 2025-06-06 -
NCT02139007 Osteoporosis PHASE4 COMPLETED 2025-07-16 University of Alabama at Birmi... More >>ngham, Birmingham, Alabama, 35294, United States Less <<
NCT00177619 Prostatic Neoplasms PHASE3 COMPLETED 2025-12-05 University of Pittsburgh, Pitt... More >>sburgh, Pennsylvania, 15213, United States Less <<
NCT01657162 Postmenopausal Osteoporosis PHASE3 COMPLETED 2016-10-03 Lakewood, Colorado, United Sta... More >>tes|Hialeah, Florida, United States|Bethesda, Maryland, United States|Buenos Aires, Argentina|Brasilia, Brazil|Curitiba, Brazil|Rio de Janeiro, Brazil|S?o Paulo, Brazil|Vitoria, Brazil|Brno, Czechia|Pardubice, Czechia|Vinohrady, Czechia|Aalborg, Denmark|Ballerup, Denmark|Vejle, Denmark|Tallinn, Estonia|Tartu, Estonia|Hong Kong, Hong Kong|Vilnius, Lithuania|Bialystok, Poland|Kielce, Poland|Lodz, Poland|Warsaw, Poland|Zgierz, Poland|Bucharest, Romania Less <<
NCT00221312 Perimenopausal Bone Loss COMPLETED 2025-07-07 University of California, San ... More >>Francisco, San Francisco, California, 94143, United States Less <<
NCT00001720 Osteoporosis PHASE2 COMPLETED 2025-06-03 National Institute of Child He... More >>alth and Human Development (NICHD), Bethesda, Maryland, 20892, United States Less <<
NCT02781805 Breast Neoplasms PHASE1 TERMINATED 2018-12-12 University of Wisconsin Carbon... More >>e Cancer Center, Madison, Wisconsin, 53705, United States Less <<
NCT00346190 Osteoporosis PHASE3 UNKNOWN 2025-04-07 Mcgill University Health cente... More >>r, Montreal, Quebec, H3A 1A1, Canada Less <<
NCT00006180 Depression|Healthy|Osteopenia|... More >>Osteoporosis Less << PHASE4 COMPLETED 2007-01-19 National Institutes of Health ... More >>Clinical Center, 9000 Rockville Pike, Bethesda, Maryland, 20892, United States Less <<
NCT00460057 Osteoporosis PHASE4 COMPLETED 2025-02-07 -
NCT02303873 Osteogenesis Imperfecta PHASE4 COMPLETED 2025-08-14 -
NCT00265252 Non-Traumatic Osteonecrosis PHASE4 UNKNOWN 2025-06-08 Kaohsiung Medical University C... More >>hung-Ho Memorial Hospital, Kaohsiung, 807, Taiwan Less <<
NCT00236002 Osteoporosis PHASE3 TERMINATED 2025-08-09 -

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.08mL

0.62mL

0.31mL

15.38mL

3.08mL

1.54mL

30.76mL

6.15mL

3.08mL

Dissolving Methods
The prepared working fluid is recommended to be prepared now and used up as soon as possible in a short period of time. The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1

References

[1]Bergstrom JD, Bostedor RG, et al. Alendronate is a specific, nanomolar inhibitor of farnesyl diphosphate synthase. Arch Biochem Biophys. 2000 Jan 1;373(1):231-41.

[2]Fisher JE, Rogers MJ, et al. Alendronate mechanism of action: geranylgeraniol, an intermediate in the mevalonate pathway, prevents inhibition of osteoclast formation, bone resorption, and kinase activation in vitro. Proc Natl Acad Sci U S A. 1999 Jan 5;96(1):133-8.

[3]Kim HY, Kim DK, Bae SH, Gwak H, Jeon JH, Kim JK, Lee BI, You HJ, Shin DH, Kim YH, Kim SY, Han SS, Shim JK, Lee JH, Kang SG, Jang H. Farnesyl diphosphate synthase is important for the maintenance of glioblastoma stemness. Exp Mol Med. 2018 Oct 17;50(10):1-12. doi: 10.1038/s12276-018-0166-2. PMID: 30333528; PMCID: PMC6193020.

[4]Bergstrom JD, Bostedor RG, Masarachia PJ, Reszka AA, Rodan G. Alendronate is a specific, nanomolar inhibitor of farnesyl diphosphate synthase. Arch Biochem Biophys. 2000 Jan 1;373(1):231-41. doi: 10.1006/abbi.1999.1502. PMID: 10620343.

[5]Black DM, Cummings SR, Karpf DB, Cauley JA, Thompson DE, Nevitt MC, Bauer DC, Genant HK, Haskell WL, Marcus R, Ott SM, Torner JC, Quandt SA, Reiss TF, Ensrud KE. Randomised trial of effect of alendronate on risk of fracture in women with existing vertebral fractures. Fracture Intervention Trial Research Group. Lancet. 1996 Dec 7;348(9041):1535-41. doi: 10.1016/s0140-6736(96)07088-2. PMID: 8950879.

[6]Saag KG, Emkey R, Schnitzer TJ, Brown JP, Hawkins F, Goemaere S, Thamsborg G, Liberman UA, Delmas PD, Malice MP, Czachur M, Daifotis AG. Alendronate for the prevention and treatment of glucocorticoid-induced osteoporosis. Glucocorticoid-Induced Osteoporosis Intervention Study Group. N Engl J Med. 1998 Jul 30;339(5):292-9. doi: 10.1056/NEJM199807303390502. PMID: 9682041.

[7]Jackson NM, Kocarek TA. Suppression of CYP2B induction by alendronate-mediated farnesyl diphosphate synthase inhibition in primary cultured rat hepatocytes. Drug Metab Dispos. 2008 Oct;36(10):2030-6. doi: 10.1124/dmd.108.022558. Epub 2008 Jul 10. PMID: 18617600; PMCID: PMC2559974.

 

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