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Alendronate

Cat. No. M3272
Alendronate Structure
Synonym:

Alendronate; MK 217; G-704650 Adronat

Size Price Availability Quantity
50mg USD 40  USD40 In stock
100mg USD 60  USD60 In stock
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Quality Control & Documentation
Biological Activity

Alendronate (Fosamax) is a farnesyl diphosphate synthase inhibitor with IC50 of 460 nM. It is a nitrogen-containing bisphosphate that acts as a robust inhibitor of bone resorption and induces apoptosis in osteoclasts. It causes disruption of the ruffled border and actin cytoskeleton of osteoclasts and induces in vitro apoptosis of osteoclasts and macrophages by inhibiting farnesyl diphosphate synthase (IC50 = 460 nM). It efficiently chelates metal ions and functions as a broad-spectrum MMP inhibitor (IC50 ~ 40 - 70 uM). And it also displays antimetastatic, anti-invasive and cell-adhesion-promoting properties (IC50 ~ 1 pM, in vitro invasion of prostate cancer cells).

Chemical Information
Molecular Weight 326.13
Formula C4H13NO7P2.3H2O.Na
CAS Number 121268-17-5
Solubility (25°C) Water 10 mg/mL warmed
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Gennady Ananchenko, et al. Alendronate sodium

[2] W P Olszynski, et al. Alendronate for the treatment of osteoporosis in men

[3] Neil A Reynolds, et al. Alendronate/colecalciferol

[4] A G Porras, et al. Pharmacokinetics of alendronate

[5] D M Black, et al. Randomised trial of effect of alendronate on risk of fracture in women with existing vertebral fractures. Fracture Intervention Trial Research Group

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Keywords: Alendronate, Alendronate; MK 217; G-704650 Adronat supplier, inhibitors, activators


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