An FPP synthase inhibitor
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Alendronate (sodium hydrate)

Item No. 13642

Technical Information
Formal Name
P,P'-(4-amino-1-hydroxybutylidene)bis-phosphonic acid, monosodium salt trihydrate (1:1:3)
CAS Number
121268-17-5
Synonyms
  • Adronat
  • Fosamax
  • G-704650
  • MK-217
Molecular Formula
C4H12NO7P2 • H6NaO3
Formula Weight
Purity
≥95%
Formulation
A crystalline solid
PBS (pH 7.2): 0.25 mg/ml
SMILES
NCCCC(P(O)([O-])=O)(O)P(O)(O)=O.[Na+]
InChi Code
InChI=1S/C4H13NO7P2.Na/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);/q;+1/p-1
InChi Key
CAKRAHQRJGUPIG-UHFFFAOYSA-M
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    Alendronate is an amino bisphosphonate that inhibits farnesyl pyrophosphate (FPP) synthase (IC50 = 50 nM for the recombinant human enzyme).1 It inhibits bone resorption in a pit formation assay using isolated rat osteoclasts (IC50 = 2 nM).2 Alendronate (3 and 10 µM) reduces angiotensin II-induced collagen I synthesis in isolated rat cardiac fibroblasts.3 It prevents femoral bone mineral density loss in ovariectomized rats when administered at a dose of 5 mg/kg.4 Formulations containing alendronate have been used in the treatment of osteoporosis and Paget's disease.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Dunford, J.E., Thompson, K., Coxon, F.P., et alStructure-activity relationships for inhibition of farnesyl diphosphate synthase in vitro and inhibition of bone resorption in vivo by nitrogen-containing bisphosphonates. J. Pharmacol. Exp. Ther. 296(2), 235-242 (2001).

    2. Sahni, M., Guenther, H.L., Fleisch, H., et alBisphosphonates act on rat bone resorption through the mediation of osteoblasts. J. Clin. Invest. 91(5), 2004-2011 (1993).

    3. Ye, Y., Lv, X., Wang, M.-h., et alAlendronate prevents angiotensin II-induced collagen I production through geranylgeranylation-dependent RhoA/Rho kinase activation in cardiac fibroblasts. J. Pharmacol. Sci. 129(4), 205-209 (2015).

    4. Azuma, Y., Oue, Y., Kanatani, H., et alEffects of continuous alendronate treatment on bone mass and mechanical properties in ovariectomized rats: Comparison with pamidronate and etidronate in growing rats. J. Pharmacol. Exp. Ther. 286(1), 128-135 (1998).