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Alendronate sodium hydrate

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Chemical Structure| 121268-17-5 同义名 : 阿仑膦酸钠三水合物 ;Alendronate;MK 217;Fosamax;Adronat;Alendronate (sodium hydrate);G-704650;Alendronate sodium trihydrate;G-704650 Adronat
CAS号 : 121268-17-5
货号 : A136794
分子式 : C4H18NNaO10P2
纯度 : 98%
分子量 : 325.124
MDL号 : MFCD01748233
存储条件：

粉末 Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

H2O: 28 mg/mL(86.12 mM)
动物实验配方：
生物活性
描述 Farnesyl diphosphate synthase (FDPS), a key enzyme in isoprenoid biosynthesis, catalyzes the conversion of isopentenyl pyrophosphate and dimethylallyl pyrophosphate to geranyl pyrophosphate and farnesyl pyrophosphate, which are protein prenylation substrates[3]. Alendronate, a nitrogen-containing bisphosphonate, is an inhibitor of farnesyl diphosphate synthase with IC50 of 460 nM, used for the treatment and prevention of osteoporosis[4]. Women with low femoral-neck bone mineral density received alendronate therapy (initially 5 mg daily, increased to 10 mg daily at 24 months) showed lower frequency of morphometric and clinical vertebral fractures[5]. Patients with osteoporosis received 5 and 10 mg of alendronate per day showed increased bone density of the lumbar spine by 2.1 ± 0.3 percent and 2.9 ± 0.3 percent, respectively, in comparison with placebo group[6]. Alendronate at 60 and 100 μM completely suppressed squalestatin 1-mediated CYP2B mRNA induction that effectively inhibited cellular farnesyl diphosphate synthase activity, and also partially suppressed phenobarbital-inducible CYP2B expression[7].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.08mL

0.62mL

0.31mL

15.38mL

3.08mL

1.54mL

30.76mL

6.15mL

3.08mL
参考文献

[1]Bergstrom JD, Bostedor RG, et al. Alendronate is a specific, nanomolar inhibitor of farnesyl diphosphate synthase. Arch Biochem Biophys. 2000 Jan 1;373(1):231-41.

[2]Fisher JE, Rogers MJ, 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.

[3]Kim HY, Kim DK, Bae SH, Gwak H, Jeon JH, Kim JK, Lee BI, You HJ, Shin DH, Kim YH, Kim SY, Han SS, Shim JK, Lee JH, Kang SG, Jang H. Farnesyl diphosphate synthase is important for the maintenance of glioblastoma stemness. Exp Mol Med. 2018 Oct 17;50(10):1-12. doi: 10.1038/s12276-018-0166-2. PMID: 30333528; PMCID: PMC6193020.

[4]Bergstrom JD, Bostedor RG, Masarachia PJ, Reszka AA, Rodan G. Alendronate is a specific, nanomolar inhibitor of farnesyl diphosphate synthase. Arch Biochem Biophys. 2000 Jan 1;373(1):231-41. doi: 10.1006/abbi.1999.1502. PMID: 10620343.

[5]Black DM, Cummings SR, Karpf DB, Cauley JA, Thompson DE, Nevitt MC, Bauer DC, Genant HK, Haskell WL, Marcus R, Ott SM, Torner JC, Quandt SA, Reiss TF, Ensrud KE. Randomised trial of effect of alendronate on risk of fracture in women with existing vertebral fractures. Fracture Intervention Trial Research Group. Lancet. 1996 Dec 7;348(9041):1535-41. doi: 10.1016/s0140-6736(96)07088-2. PMID: 8950879.

[6]Saag KG, Emkey R, Schnitzer TJ, Brown JP, Hawkins F, Goemaere S, Thamsborg G, Liberman UA, Delmas PD, Malice MP, Czachur M, Daifotis AG. Alendronate for the prevention and treatment of glucocorticoid-induced osteoporosis. Glucocorticoid-Induced Osteoporosis Intervention Study Group. N Engl J Med. 1998 Jul 30;339(5):292-9. doi: 10.1056/NEJM199807303390502. PMID: 9682041.

[7]Jackson NM, Kocarek TA. Suppression of CYP2B induction by alendronate-mediated farnesyl diphosphate synthase inhibition in primary cultured rat hepatocytes. Drug Metab Dispos. 2008 Oct;36(10):2030-6. doi: 10.1124/dmd.108.022558. Epub 2008 Jul 10. PMID: 18617600; PMCID: PMC2559974.