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KI0779Risedronate sodium50 mg$154

Chemical Characteristic

Product NameRisedronate sodium
SynonymsActonel
CAS No.115436-72-1
Molecular Weight 305.09
FormulaC7H10NNaO7P2
Chemical Structure

Biological activities

Risedronate sodium is sodium of risedronate. Risedronate sodium is an orally active antiresorptive agent and is one of the most potent bisphosphonates. Risedronate sodium has been approved for the treatment of Paget閳ユ獨 disease of the bone and is under development as a chronic therapy for the treatment and prevention of osteoporosis.[1] Risedronate inhibits recombinant farnesyl diphosphate synthase with an IC50 of 3.9 nM. [2] The IC50 of risedronate for the LM8, SaOS2 and KHOS cells after 72 hours exposure are 3.7, 3.8 and 4.3 µM, respectively. Risedronate inhibits both prenylation of Rap1A and Ras and phosphorylation of Erk 1 and 2 at a dose of 50 µM for 48 hours. Risedronate induces apoptosis and inhibits the growth of osteogenic sarcoma through a mechanism involving the down-regulation of protein prenylation. Risedronate treatment also increases intranucleosomal genomic DNA fragmentation. Risedronate augments the effects of carboplatin, doxorubicin, vincristine and etoposide synergistically across a wide range of fractions affected (Fa) values. Treatment with risedronate induces significant time- and dose-dependent cytotoxicity in the LM8 cell line. [3] Risedronate sodium is against blood stages of Plasmodium falciparum with an IC50 of 20.3 µM. Risedronate inhibits the transfer of the farnesyl pyrophosphate group to parasite proteins. [4] In vivo, risedronate leads to an 88.9% inhibition of the rodent parasite Plasmodium berghei in mice on the seventh day of treatment. [2]

Protocols

Risedronate is dissolved in sterile deionized water, resulting in a 25 mM stock solution. [2]

References

[1] Perkins AC, et al. Esophageal transit of risedronate cellulose-coated tablet and gelatin capsule formulations. Int J Pharm. 1999, 186(2): 169-175. 閵嗏偓閵嗏偓
[2] Bergstrom JD, et al. Alendronate is a specific, nanomolar inhibitor of farnesyl diphosphate synthase. Arch Biochem Biophys. 2000, 373(1): 231-241. 閵嗏偓閵嗏偓
[3] Murayama T, et al. Efficacy of the third-generation bisphosphonate risedronate alone and in combination with anticancer drugs against osteosarcoma cell lines. Anticancer Res. 2008, 28(4B): 2147-2154. 閵嗏偓閵嗏偓
[4] Jord?o FM, et al. In vitro and in vivo antiplasmodial activities of risedronate and its interference with protein prenylation in Plasmodium falciparum. Antimicrob Agents Chemother. 2011, 55(5): 2026-2031. 閵嗏偓閵嗏偓

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