Zoledronic AcidPotent nitrogen-containing bisphosphonates CAS# 118072-93-8 |
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| Cas No. | 118072-93-8 | SDF | Download SDF |
| PubChem ID | 68740 | Appearance | Powder |
| Formula | C5H10N2O7P2 | M.Wt | 272.09 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Synonyms | Zoledronate; CGP 42446; CGP42446A; ZOL 446 | ||
| Solubility | Soluble to 40 mg/mL (147.01 mM) in 0.1M NaOH (aq) | ||
| Chemical Name | (1-hydroxy-2-imidazol-1-yl-1-phosphonoethyl)phosphonic acid | ||
| SMILES | C1=CN(C=N1)CC(O)(P(=O)(O)O)P(=O)(O)O | ||
| Standard InChIKey | XRASPMIURGNCCH-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C5H10N2O7P2/c8-5(15(9,10)11,16(12,13)14)3-7-2-1-6-4-7/h1-2,4,8H,3H2,(H2,9,10,11)(H2,12,13,14) | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | Potent bisphophonate farnesyl diphosphate (FPP) synthase inhibitor (IC50 = 20 nM). Inhibits osteoclast-mediated bone resorption. Also inhibits Ras signaling and tumor growth, and induces apoptosis in pancreatic cancer cells. Reverses epithelial-mesenchymal transition and inhibits breast cancer cell renewal via inactivation of NF-κB. |
Zoledronic Acid Dilution Calculator
Zoledronic Acid Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 3.6753 mL | 18.3763 mL | 36.7525 mL | 73.5051 mL | 91.8814 mL |
| 5 mM | 0.7351 mL | 3.6753 mL | 7.3505 mL | 14.701 mL | 18.3763 mL |
| 10 mM | 0.3675 mL | 1.8376 mL | 3.6753 mL | 7.3505 mL | 9.1881 mL |
| 50 mM | 0.0735 mL | 0.3675 mL | 0.7351 mL | 1.4701 mL | 1.8376 mL |
| 100 mM | 0.0368 mL | 0.1838 mL | 0.3675 mL | 0.7351 mL | 0.9188 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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Zoledronic acid, one of the most potent nitrogen-containing bisphosphonates, induces anti-proliferative and apoptotic effects on multiple myeloma cell lines in vitro by activating protein kinase C. Zoledronic acid also inhibits proliferation of human foet
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Zoledronic acid improves bone histomorphometry in a murine model of Rett syndrome.[Pubmed:28323142]
Bone. 2017 Jun;99:1-7.
Rett syndrome (RTT) is a neurodevelopmental disorder predominately affecting young females, caused by deficiency of the global transcriptional protein methyl CpG binding protein 2 (MeCP2). Osteoblasts express MeCP2 and girls with RTT experience early onset osteoporosis, decreased bone mass and an increased fracture risk. There is no defined treatment for osteoporosis associated with RTT. The present study evaluated the effects of Zoledronic Acid (ZA), a third generation nitrogen-containing bisphosphonate with primarily anti-osteoclastic activity, in a mouse model of MeCP2 deficiency. Mice received weekly injections of 20mug/kg ZA for six weeks. Due to the shortened lifespan of hemizygous male (Mecp2-null) mice, treatment began at 3weeks of age for this group and corresponding wildtype (WT) male mice. Treatment for heterozygous (HET) and WT female mice began at 8weeks of age. Micro-computed tomography (micro-CT) and dynamic analyses of bone turnover were performed. ZA treatment led to significant increases in bone volume fraction, number, connectivity density and apparent density of trabecular bone in all genotypes of mice. In contrast, cortical bone generally was unaffected by ZA injections. Parameters of bone turnover, including mineral apposition rate, labeled bone surface and bone formation rate decreased after treatment with ZA. Mecp2-null mice had reduced labeled bone surface and bone formation rate compared to WT male mice. The results indicate that ZA treatment significantly improved trabecular bone mass in a murine model of RTT with little effect on cortical bone.
Zoledronic acid boosts gammadelta T-cell activity in children receiving alphabeta(+) T and CD19(+) cell-depleted grafts from an HLA-haplo-identical donor.[Pubmed:28344861]
Oncoimmunology. 2016 Sep 27;6(2):e1216291.
We demonstrated that gammadelta T cells of patients given HLA-haploidentical HSCT after removal of alphabeta(+) T cells and CD19(+) B cells are endowed with the capacity of killing leukemia cells after ex vivo treatment with Zoledronic Acid (ZOL). Thus, we tested the hypothesis that infusion of ZOL in patients receiving this type of graft may enhance gammadelta T-cell cytotoxic activity against leukemia cells. ZOL was infused every 28 d in 43 patients; most were treated at least twice. gammadelta T cells before and after ZOL treatments were studied in 33 of these 43 patients, till at least 7 mo after HSCT by high-resolution mass spectrometry, flow-cytometry, and degranulation assay. An induction of Vdelta2-cell differentiation, paralleled by increased cytotoxicity of both Vdelta1 and Vdelta2 cells against primary leukemia blasts was associated with ZOL treatment. Cytotoxic activity was further increased in Vdelta2 cells, but not in Vdelta1 lymphocytes in those patients given more than one treatment. Proteomic analysis of gammadelta T cells purified from patients showed upregulation of proteins involved in activation processes and immune response, paralleled by downregulation of proteins involved in proliferation. Moreover, a proteomic signature was identified for each ZOL treatment. Patients given three or more ZOL infusions had a better probability of survival in comparison to those given one or two treatments (86% vs. 54%, respectively, p = 0.008). Our data indicate that ZOL infusion in pediatric recipients of alphabeta T- and B-cell-depleted HLA-haploidentical HSCT promotes gammadelta T-cell differentiation and cytotoxicity and may influence the outcome of patients.
