FSL0337

Structure

• InChI=1S/C4H13NO7P2/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)
• InChIKey=OGSPWJRAVKPPFI-UHFFFAOYSA-N

Synonyms

• 66376-36-1
• Alendronate

Origin

Chemically synthesized

Biological activities

Inhibition of the prenylation of small GTP-binding proteins in osteoclasts and disruption of their cytoskeleton.

Therapeutic

Malignant
Paget's disease bone
Postmenopausal osteoporosis

Target

Farnesyl pyrophosphate synthase (FPPS)

Assay information

Inhibition of the enzymatic activity of recominant human FPP synthase (IC₅₀ = 460 nM), which generates isoprenoid lipids used for the posttranslational modification of small GTP-binding proteins essential for osteoclast function
Inhibition of the incorporation of [³H]-mevalonolactone both into prenylated proteins and into nonsaponifiable lipids in osteoclasts (IC₅₀ = 15 μM)
Prevention of early trabecular bone loss and cartilage degeneration following non-invasive knee injury using mice assay (1000 μg/kg/dose as high-dose alendronate treatment )
Increase in sensitivity of Huh-7 HCC cell against the drug-combination (5 μM alendronate + 30 μM 5'-azacytizine)