Ibandronic acidCAS# 114084-78-5 |
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Quality Control & MSDS
3D structure
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| Cas No. | 114084-78-5 | SDF | Download SDF |
| PubChem ID | 6331794 | Appearance | Powder |
| Formula | C9H23NO7P2 | M.Wt | 319.23 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | Soluble in DMSO | ||
| Chemical Name | [1-hydroxy-3-[methyl(pentyl)amino]-1-phosphonopropyl]phosphonic acid;sodium | ||
| SMILES | CCCCCN(C)CCC(O)(P(=O)(O)O)P(=O)(O)O.[Na] | ||
| Standard InChIKey | WQVSHLXLXKMYEW-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C9H23NO7P2.Na/c1-3-4-5-7-10(2)8-6-9(11,18(12,13)14)19(15,16)17;/h11H,3-8H2,1-2H3,(H2,12,13,14)(H2,15,16,17); | ||
| 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 | Ibandronic acid is a highly potent nitrogen-containing bisphosphonate used for the treatment of osteoporosis.
Target: Others
Ibandronate (1.25-2 μM) significantly reduces endothelial cell growth, while ibandronate (2 μM) also significantly reduces capillary-like tube formation and increases apoptosis of endothelial cells. Ibandronate (< 100 μM) dose-dependently increases VEGF expression in endothelial cells [1]. Ibandronate (< 100 μM) inhibits growth of both prostate cancer cell lines (LNCaP and PC-3) in a dose dependent manner [2].
Ibandronate administered either daily (2.5 mg) or intermittently (20 mg every other day for 12 doses every 3 months) significantly reduces the risk of new morphometric vertebral fractures by 62% and 50% (p = 0.0006), respectively, in osteoporotic women after 3 years' treatment. Ibandronate administered either daily (2.5 mg) or intermittently (20 mg every other day for 12 doses every 3 months) significantly and progressively increases BMD of lumbar spine by 6.5% and 5.7%, respectively, in osteoporotic women after 3 years' treatment [3]. Ibandronate (< 125 mg/kg s.c.) results in a dose dependent increase in bone mineral density (BMD), trabecular bone volume and trabecular number, load to failure (Fmax), and yield load in long bones and vertebrae in ovariectomized rats, and increased trabecular separation in ovariectomized rats is fully prevented by all doses [4]. References: | |||||
Ibandronic acid Dilution Calculator
Ibandronic acid Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 3.1325 mL | 15.6627 mL | 31.3254 mL | 62.6508 mL | 78.3134 mL |
| 5 mM | 0.6265 mL | 3.1325 mL | 6.2651 mL | 12.5302 mL | 15.6627 mL |
| 10 mM | 0.3133 mL | 1.5663 mL | 3.1325 mL | 6.2651 mL | 7.8313 mL |
| 50 mM | 0.0627 mL | 0.3133 mL | 0.6265 mL | 1.253 mL | 1.5663 mL |
| 100 mM | 0.0313 mL | 0.1566 mL | 0.3133 mL | 0.6265 mL | 0.7831 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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Ibandronic acid is a highly potent nitrogen-containing bisphosphonate used for the treatment of osteoporosis.
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Bioequivalence study of two formulations of ibandronic acid 150-mg film-coated tablets in healthy volunteers under fasting conditions: a randomized, open-label, three-way, reference-replicated crossover study.[Pubmed:24756462]
Drugs R D. 2014 Jun;14(2):105-12.
AIMS: This bioequivalence study aimed to compare rate and extent of absorption of a generic medicinal product of Ibandronic acid 150-mg film-coated tablet versus Bonviva((R)). METHODS: This was a single-centre, open-label, randomized, three-way, three-sequence, reference-replicated, crossover bioequivalence study, under fasting conditions. A single oral dose of Ibandronic acid as one 150-mg film-coated tablet was administered in each study period. Each washout period lasted 14 days. Blood samples were collected according to a predefined sampling schedule and up to 48.0 hours after administraton in each period. Plasma concentrations of Ibandronic acid were measured using a liquid chromatograph-mass spectrometry/mass spectrometry method. Bioequivalence between generic and reference medicinal products is acceptable if the 90 % confidence intervals (CI) of ratio of least-squares means between the test and the reference product of ln-transformed area under the serum concentration-time curve from time zero to time of last measurable concentration (AUC0-t ) is within the 80.00-125.00 % interval. Prospectively, a scaled average bioequivalence approach for maximum serum concentration (C max) was established. RESULTS: 153 healthy volunteers were enrolled and randomized. After the test formulation (T) and first and second Bonviva((R)) (R) dosing, the C max was 96.71 +/- 90.19 ng/mL, 92.67 +/- 91.48 ng/mL and 87.94 +/- 60.20 ng/mL and the AUC0-t was 390.83 +/- 287.27 ng.h/mL, 388.54 +/- 356.76 ng.h/mL and 383.53 +/- 246.72, respectively. Ratios of T/R and 90 % CI were 100.92 % (94.35-107.94) for AUC0-t , 100.90 % (94.37-107.88) for AUC0-inf and 102.56 % (95.05-110.67) for C max. CONCLUSIONS: Test formulation of Ibandronic acid is bioequivalent in rate and extent of absorption to Bonviva((R)) following a 150-mg dose, under fasting conditions.
Oral ibandronic acid versus intravenous zoledronic acid in treatment of bone metastases from breast cancer: a randomised, open label, non-inferiority phase 3 trial.[Pubmed:24332514]
Lancet Oncol. 2014 Jan;15(1):114-22.
BACKGROUND: Bisphosphonates are routinely used in the treatment of metastatic bone disease from breast cancer to reduce pain and bone destruction. Zoledronic acid given by intravenous infusion has been widely used, but places a substantial logistical burden on both patient and hospital. As a result, the use of oral Ibandronic acid has increased, despite the absence of comparative data. In the ZICE trial, we compared oral Ibandronic acid with intravenous zoledronic acid for the treatment of metastatic breast cancer to bone. METHODS: This phase 3, open-label, parallel group active-controlled, multicentre, randomised, non-inferiority phase 3 study was done in 99 UK hospitals. Eligibility criteria included at least one radiologically confirmed bone metastasis from a histologically confirmed breast cancer. Patients with ECOG performance status 0 to 2 and clinical decision to treat with bisphosphonates within 3 months of randomisation were randomly assigned to receive 96 weeks of treatment with either intravenous zoledronic acid at 4 mg every 3-4 weeks or oral Ibandronic acid 50 mg daily. Randomisation (1:1) was done via a central computerised system within stratified block sizes of four. Randomisation was stratified on whether patients had current or planned treatment with chemotherapy; current or planned treatment with hormone therapy; and whether they had a previous skeletal-related event within the last 3 months or had planned radiotherapy treatment to the bone or planned orthopaedic surgery due to bone metastases. The primary non-inferiority endpoint was the frequency and timing of skeletal-related events over 96 weeks, analysed using a per-protocol analysis. All active (non-withdrawn) patients have now reached the 96-week timepoint and the trial is now in long-term follow-up. The trial is registered with ClinicalTrials.gov, number NCT00326820. FINDINGS: Between Jan 13, 2006, and Oct 4, 2010, 705 patients were randomly assigned to receive Ibandronic acid and 699 to receive zoledronic acid; three patients withdrew immediately after randomisation. The per-protocol analysis included 654 patients in the Ibandronic acid group and 672 in the zoledronic acid group. Annual rates of skeletal-related events were 0.499 (95% CI 0.454-0.549) with Ibandronic acid and 0.435 (0.393-0.480) with zoledronic acid; the rate ratio for skeletal-related events was 1.148 (95% CI 0.967-1.362). The upper CI was greater than the margin of non-inferiority of 1.08; therefore, we could not reject the null hypothesis that Ibandronic acid was inferior to zoledronic acid. More patients in the zoledronic acid group had renal toxic effects than in the Ibandronic acid group (226 [32%] of 697 vs 172 [24%] of 704) but rates of osteonecrosis of the jaw were low in both groups (nine [1%] of 697 vs five [<1%] of 704). The most common grade 3 or 4 adverse events were fatigue (97 [14%] of 697 patients allocated zoledronic acid vs 98 [14%] of 704 allocated Ibandronic acid), increased bone pain (91 [corrected] [13%] vs 85 [corrected] [12%]), joint pain (41 [corrected] [6%] vs 38 [5%]), infection (31 [5%] vs 23 [corrected] [3%]), and nausea or vomiting (38 [5%] vs 41 [6%]). INTERPRETATION: Our results suggest that zoledronic acid is preferable to Ibandronic acid in preventing skeletal-related events caused by bone metastases. However, both drugs have acceptable side-effect profiles and the oral formulation is more convenient, and could still be considered if the patient has a strong preference or if difficulties occur with intravenous infusions. FUNDING: Roche Products Ltd (educational grant), supported by National Institute for Health Research Cancer Network, following endorsement by Cancer Research UK (CRUKE/04/022).
Ventricular tachycardia-based long QT without hypocalcaemia after use of ibandronic acid.[Pubmed:24217211]
Cardiovasc J Afr. 2013 Jun 23;24(5):e11-4.
Many drugs are known to cause lengthening of the QT interval. Ibandronic acid is a frequently used agent in the treatment of osteoporosis and is known to cause prolongation of the QT interval due to hypocalcaemia. However, no cases of long QT syndrome associated with ventricular tachycardia (VT) with a serum calcium level within the normal limits have been reported in the literature. We report on a case of a VT-based long QT syndrome associated with the use of Ibandronic acid.
Modulating effect of matrices with calcium phosphate coating on cytotoxicity of strontium ranelate and ibandronic acid in vitro.[Pubmed:24958373]
Bull Exp Biol Med. 2014 Jun;157(2):215-9.
Strontium ranelate (29 mug/ml) and Ibandronic acid (50 muM) produced a cytotoxic effect on rat bone marrow myelokaryocytes in vitro. Strontium ranelate increased the number of myelokaryocytes with signs of necrosis, Ibandronic acid increased the number of apoptotic and necrotic cells in the 9-day 2D culture of bone marrow cells on the plastic surface of the wells of culture plates. Co-culturing of the bone marrow with 3D matrices with microarc calcium phosphate coating that simulated bone mineral matrix increased intracellular ROS concentration, but abolished the cytotoxic effect of these drugs.
