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Purity: ≥98%
Alendronate sodium hydrate, the sodium salt of alendronate, is a novel and potent farnesyl diphosphate synthase inhibitor with IC50 of 460 nM. Alendronate sodium is a second generation bisphosphonate and synthetic analog of pyrophosphate with bone anti-resorption activity. Alendronate sodium binds to and inhibits the activity of geranyltranstransferase (farnesyl pyrophosphate synthetase), an enzyme involved in terpenoid biosynthesis. Inhibition of this enzyme prevents the biosynthesis of isoprenoid lipids (FPP and GGPP) that are donor substrates of farnesylation and geranylgeranylation during the post-translational modification of small GTPase signalling proteins, which is important in the process of osteoclast turnover. As a result, osteoclast activity is inhibited and bone resorption and turnover are reduced.
| ln Vitro |
The rate-limiting stage of phospholipid production, which is essential for osteoclast function, is inhibited by alendronate sodium hydrate when it directly acts on osteoclasts [1]. Alendronate Sodium Hydrate dose-dependently inhibits [3H]MVA uptake of sterols, with concurrent increases in dose markers for IPP and DMAPP [3]. Alendronate Sodium Hydrate inhibits [3H]mevalonolactone due to reduced levels of geranylgeranyl diphosphate, a protein of 18–25 kDa and a non-saponifiable inhibitor, including sterols in osteoclasts [2].
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| ln Vivo |
In rabbits, alendronate sodium hydrate results in gastric erosion but not the development of gastric antrums. The frequency and magnitude of stomach antrums caused by caromethacin are increased by alendronate sodium hydrate. Gastric healing is delayed and the effects of the carbohydrate carotethacin are amplified by alendronate sodium hydrate [4]. When combined with paclitaxel (10–50 mg/kg/day twice or twice a day), alendronate sodium hydrate (0.04-0.1 mg/kg twice weekly or 0.1 mg/kg weekly) partially inhibits the bone metastasis of human PC-3 ML cells in mice treated with it. This can lead to a fatal outbreak of tumor growth of PC-3 ML in bone marrow and soft tissue, but the rate is significantly improved within 4-5 weeks [5].
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| References |
[1]. Fisher JE, et al. Alendronate mechanism of action: geranylgeraniol, an intermediate in the mevalonate pathway, prevents inhibition of osteoclast formation, bone resorption, and kinase activation in vitro. Proc Natl Acad Sci U S A. 1999 Jan 5;96(1):133-8
[2]. Bergstrom JD, et al. Alendronate is a specific, nanomolar inhibitor of farnesyl diphosphate synthase. Arch Biochem Biophys. 2000 Jan 1;373(1):231-41. [3]. Keller RK, et al. Mechanism of aminobisphosphonate action: characterization of alendronate inhibition of the isoprenoid pathway. Biochem Biophys Res Commun. 1999 Dec 20;266(2):560-3. [4]. Elliott SN, et al. Alendronate induces gastric injury and delays ulcer healing in rodents. Life Sci. 1998;62(1):77-91. [5]. Stearns ME, et al. Effects of alendronate and taxol on PC-3 ML cell bone metastases in SCID mice. Invasion Metastasis. 1996;16(3):116-31 |
| Molecular Formula |
C4H18NNAO10P2
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|---|---|
| Molecular Weight |
325.1237
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| CAS # |
121268-17-5
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| Related CAS # |
Alendronic acid;66376-36-1;Alendronic acid-d6;1035437-39-8;Alendronate sodium;129318-43-0
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| SMILES |
OC(P([O-])(O)=O)(P(O)(O)=O)CCCN.[H]O[H].[H]O[H].[H]O[H].[Na+]
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| InChi Key |
DCSBSVSZJRSITC-UHFFFAOYSA-M
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| InChi Code |
InChI=1S/C4H13NO7P2.Na.3H2O/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);;3*1H2/q;+1;;;/p-1
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| Chemical Name |
(4-amino-1-hydroxybutylidene) bisphosphonic acid monosodium salt trihydrate.
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| Synonyms |
MK 217; MK-217; G-704650 Adronat; Alendronate; Alendronic Acid Monosodium Salt Trihydrate. trade names: Fosamax; Adronat; Alendros; Onclast. Code names: G704650; MK217.
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
H2O : ≥ 28.57 mg/mL (~87.88 mM)
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| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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