| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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Purity: ≥98%
Neridronate (also known as Neridronic acid) is an aminobisphosphonate used in Italy for the treatment of osteogenesis imperfecta (OI) and Paget’s disease of bone (PDB). Neridronate is effective also in other skeletal diseases such as osteoporosis, algodystrophy, hypercalcemia of malignancy, and bone metastases. Neridronic acid, also known neridronate, is a bisphosphonate. Neridronic acid treatment has been reported to be effective also in other skeletal diseases such as osteoporosis, algodystrophy, hypercalcemia of malignancy and bone metastasis. Neridronic acid has been developed only for parenteral use, and it is the only one used as intramuscular injection.
| References | |
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| Additional Infomation |
Neridronic acid is a 1,1-bis(phosphonic acid).
Neridronic Acid is a third-generation, aminohexane bisphosphonate with anti-resorptive and anti-hypercalcemic activities. Although the exact mechanism of action has yet to be fully elucidated, neridronic acid binds to and adsorbs onto hydroxyapatite crystals in bone matrix, thereby preventing osteoclast resorption. This agent also binds to and inhibits farnesyl pyrophosphate synthase, an enzyme that plays an important role in the mevalonate pathway. This inhibits the formation of isoprenoids that are substrates for protein prenylation. This prevents farnesylation and geranylgeranylation of proteins essential for osteoclast function, thereby leading to the induction of apoptosis of osteoclasts. By preventing osteoclast-mediated bone resorption, neridronic acid decreases bone turnover rate, stabilizes the bone matrix and reduces hypercalcemia. |
| Molecular Formula |
C6H17NO7P2
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|---|---|
| Molecular Weight |
277.14928
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| Exact Mass |
277.048
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| CAS # |
79778-41-9
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| Related CAS # |
80729-79-9 (sodium);79778-41-9 (free acid);
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| PubChem CID |
71237
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| Appearance |
White to off-white solid powder
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| Density |
1.7±0.1 g/cm3
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| Boiling Point |
600.1±65.0 °C at 760 mmHg
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| Melting Point |
245°
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| Flash Point |
316.7±34.3 °C
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| Vapour Pressure |
0.0±3.9 mmHg at 25°C
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| Index of Refraction |
1.569
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| LogP |
-3.36
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| Hydrogen Bond Donor Count |
6
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
16
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| Complexity |
286
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=P(C(P(O)(O)=O)(CCCCCN)O)(O)O
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| InChi Key |
PUUSSSIBPPTKTP-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C6H17NO7P2/c7-5-3-1-2-4-6(8,15(9,10)11)16(12,13)14/h8H,1-5,7H2,(H2,9,10,11)(H2,12,13,14)
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| Chemical Name |
(6-Amino-1-hydroxyhexylidene)diphosphonic acid
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| Synonyms |
Neridronic acid; Nerixia.
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| HS Tariff Code |
2934.99.9001
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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 : ~5 mg/mL (~18.04 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2 mg/mL (7.22 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication (<60°C).
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.6082 mL | 18.0408 mL | 36.0815 mL | |
| 5 mM | 0.7216 mL | 3.6082 mL | 7.2163 mL | |
| 10 mM | 0.3608 mL | 1.8041 mL | 3.6082 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT01803360 | UNKNOWN STATUS | Drug: Neridronate | Osteoarthritis, Knee | ASST Gaetano Pini-CTO | 2013-03 | Phase 2 |
| NCT01140321 | COMPLETED | Drug: Neridronate | Osteoporosis Thalassemia Intermedia Thalassemia Major |
Ente Ospedaliero Ospedali Galliera | 2004-01 | Phase 2 |
| NCT02402530 | COMPLETED | Drug: Placebo Drug: Neridronic acid 62.5 mg |
Complex Regional Pain Syndrome, Type I | Grünenthal GmbH | 2015-04 | Phase 2 Phase 3 |
| NCT02972359 | COMPLETEDWITH RESULTS | Drug: Neridronic acid | Complex Regional Pain Syndrome | Grünenthal GmbH | 2016-12-20 | Phase 3 |
| NCT03560986 | TERMINATEDWITH RESULTS | Drug: Neridronic acid 100 mg Drug: Placebo |
Complex Regional Pain Syndrome (CRPS) | Grünenthal GmbH | 2018-05-31 | Phase 3 |
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