Zoledronic acid-d₅  (Synonyms: Zoledronate-d₅; CGP 42446-d₅; CGP42446A-d₅; ZOL 446-d₅)

Zoledronic acid-d₅ is deuterated labeled Zoledronic Acid (HY-13777). Zoledronic Acid (Zoledronate) is a third-generation bisphosphonate (BP), with potent anti-resorptive activity. Zoledronic Acid inhibits the differentiation and apoptosis of osteoclasts. Zoledronic Acid also has anti-cancer effects^[1].

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs^[1].
Zoledronic Acid (0.1-1 μM; 48 hours) increases receptor activator of nuclear factor kB ligand (RANKL) and sclerostin mRNA expressions in osteocyte-like MLO-Y4 cells^[3].
Zoledronic Acid increases the expression of osteoclastogenesis supporting factor from MLO-Y4 cells^[3].
Zoledronic Acid enhances the RANKL expression via IL-6/ JAK2/STAT3 pathway in MLO-Y4 cells^[3].
Zoledronic acid inhibits osteoclast differentiation and function through the regulation of NF-κB and JNK signalling pathways^[4].
Zoledronic Acid (10-100 μM; 1-7 days) markedly reduces the viability of MC3T3-E1 cells^[5].
Zoledronic Acid (10-100 μM; 1-7 days) induces apoptosis in MC3T3-E1 cells^[5].
Zoledronic Acid (10-100 μM; 4 days) inhibits cell viability due to the induction of apoptosis^[5].
Zoledronic Acid exerts inhibitory effects on the differentiation and maturation of MC3T3-E1 cells at concentrations <1 μM^[5].

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

Zoledronic Acid (0.05 mg/kg; i.p.; weekly; for 3 weeks) increases bone mineral density and content^[6].
Zoledronic Acid (0.5-1 mg/kg; i.p.; weekly; for 3 weeks) inhibits both osteoclast and osteoblasts function and bone remodeling in vivo interfering with bone mechanical properties^[6].

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

277.12

C₅H₅D₅N₂O₇P₂

118072-93-8

OC(P(O)(O)=O)(P(O)(O)=O)C([2H])([2H])N1C([2H])=C([2H])N=C1[2H]

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;53(2):211-216.  [Content Brief]

  [2]. Shea GKH, et al. Oral Zoledronic acid bisphosphonate for the treatment of chronic low back pain with associated Modic changes: A pilot randomized controlled trial. J Orthop Res. 2022 Feb 23.  [Content Brief]

  [3]. Lianwei Wang, et al. Various pathways of zoledronic acid against osteoclasts and bone cancer metastasis: a brief review. BMC Cancer. 2020; 20: 1059.  [Content Brief]

  [4]. Hyung Joon Kim, et al. Zoledronate Enhances Osteocyte-Mediated Osteoclast Differentiation by IL-6/RANKL Axis. Int J Mol Sci. 2019 Mar; 20(6): 1467.  [Content Brief]

  [5]. Xiao-Lin Huang, et al. Zoledronic acid inhibits osteoclast differentiation and function through the regulation of NF-κB and JNK signalling pathways. Int J Mol Med. 2019 Aug;44(2):582-592.  [Content Brief]

  [6]. XIN HUANG, et al. Dose-dependent inhibitory effects of zoledronic acid on osteoblast viability and function in vitro. Mol Med Rep. 2016 Jan; 13(1): 613-622.  [Content Brief]

  [7]. Samantha Pozzi, et al. High-dose zoledronic acid impacts bone remodeling with effects on osteoblastic lineage and bone mechanical properties. Clin Cancer Res. 2009 Sep 15;15(18):5829-39.  [Content Brief]