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Alendronate sodium hydrate (Synonyms: Alendronate; MK 217; G-704650 Adronat)

Cat. No.: HY-11101 Purity: >98.0%
Handling Instructions

Alendronate (sodium hydrate) is a farnesyl diphosphate synthase inhibitor with IC50 of 460 nM.

For research use only. We do not sell to patients.

Alendronate sodium hydrate Chemical Structure

Alendronate sodium hydrate Chemical Structure

CAS No. : 121268-17-5

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Description

Alendronate (sodium hydrate) is a farnesyl diphosphate synthase inhibitor with IC50 of 460 nM.

IC50 & Target

IC50: 460 nM (farnesyl diphosphate synthase)

In Vitro

Alendronate, acting directly on osteoclasts, inhibits a rate-limiting step in the cholesterol biosynthesis pathway, essential for osteoclast function[1]. Alendronate inhibits the isoprenoid biosynthesis pathway and interferes with protein prenylation, as a result of reduced geranylgeranyl diphosphate levels. Alendronate inhibits the incorporation of [3H]mevalonolactone into proteins of 18-25 kDa and into nonsaponifiable lipids, including sterols in osteoclasts[2]. Alendronate causes a dose-dependent inhibition of [3H]MVA incorporation into sterols and a concomitant increase in incorporation of radiolabel into IPP and DMAPP[3].

In Vivo

Alendronate causes erosions in the rabbit stomach, but not antral ulceration in rats. Alendronate increases the incidence and size of indomethacin-induced antral ulcers. Alendronate also enhances indomethacin-induced gastricdamage in the rat, and delays gastric ulcer healing[4]. Alendronate (0.04-0.1 mg/kg twice weekly or 0.1 mg/kg weekly) partially blocks the establishment of bone metastases by human PC-3 ML cells and results in tumor formation in the peritoneum and other soft tissues. Alendronate pretreatment of mice (0.1 mg/kg twice weekly or weekly) and dosing along with taxol (10-50 mg/kg/day, twice weekly, or weekly) blocks the growth of PC-3 ML tumors in the bone marrow and soft tissues in a statistically significant manner and improves survival rates significantly by 4-5 weeks[5].

Clinical Trial
Molecular Weight

325.12

Formula

C₄H₁₈NNaO₁₀P₂

CAS No.

121268-17-5

SMILES

[O-]P(C(O)(CCCN)P(O)(O)=O)(O)=O[Na+]

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

H2O : ≥ 28.57 mg/mL (87.88 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.0758 mL 15.3789 mL 30.7579 mL
5 mM 0.6152 mL 3.0758 mL 6.1516 mL
10 mM 0.3076 mL 1.5379 mL 3.0758 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Kinase Assay
[3]

Rat liver cytosol is prepared from a separate piece of liver from rat. Assays are carried out in a total volume of 0.1 mL containing 10 mg of cytosolic protein, and components according to Rilling. All reaction components (except IPP) are mixed and kept on ice for 15 min. Reactions are initiated by the addition of [14C]IPP and incubation at 37°C. Reactions are stopped after 5 min by addition of 0.4 mL MeOH/HCl (4/1, by vol.) and the samples are incubated a further 15 min to hydrolyze the allylic pyrophosphates to petroleum ether-extractable products. Following addition of 0.5 mL water and 1 mL petroleum ether, 50% of the upper (petroleum ether-extractable) phase is taken for liquid scintillation analysis. Preliminary experiments indicated that the reaction is linear with time and protein under these conditions, and no more than 10% of the substrate is consumed.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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Alendronate sodium hydrate
Cat. No.:
HY-11101
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