Olpadronic acid
Based on 1 Customer Validation
Olpadronic acid (Olpadronate) is an orally active amino-bisphosphonate and inhibits bone resorption. Olpadronic acid prevents bone destruction and tumor growth in the skeletal prostate cancer mouse model. Olpadronic acid can be used for research of osteoporosis, malignancies and rheumatoid arthritis.
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- Pureté: 95.0%
- CAS No.: 63132-39-8
- Formule: C5H15NO7P2
- Masse moléculaire:263.12
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Orally Active Compound Library
HY-L061
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Anti-Pancreatic Cancer Compound Library
HY-L077
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Human Metabolite Library
HY-L123
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Anti-Prostate Cancer Compound Library
HY-L124
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Metabolic Enzyme Compound Library
HY-L146
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Bioactive Compound Library Max
HY-L181
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MCE Bioactive Compound Library
HY-L001V
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Bioactive Compound Library
HY-L001
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High-Throughput Bioactive Compound Library
HY-L205
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Anti-Rheumatic Arthritis Compound Library
HY-L210
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Immunology/Inflammation Compound Library
HY-L007
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Metabolism/Protease Compound Library
HY-L012
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Anti-Cancer Compound Library
HY-L025
Activité biologique
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| T-cell | IC50 |
112 μM
Compound: 31
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Inhibitory activity, for stimulation of TNF-alpha release in gamma-delta T cells, using a constrained maximum TNF-alpha release of 2700 pg/mL
Inhibitory activity, for stimulation of TNF-alpha release in gamma-delta T cells, using a constrained maximum TNF-alpha release of 2700 pg/mL
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[PMID: 14711309] |
| T-cell | IC50 |
46 μM
Compound: 31
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Inhibitory activity, for stimulation of TNF-alpha release in gamma-delta T cells, using individual observed maximum TNF-alpha release
Inhibitory activity, for stimulation of TNF-alpha release in gamma-delta T cells, using individual observed maximum TNF-alpha release
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[PMID: 14711309] |
| Vero | IC50 |
>200 μM
Compound: 19
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Inhibition of Trypanosoma cruzi Amastigotes was determined in Vero cells culture and fetal calf serum
Inhibition of Trypanosoma cruzi Amastigotes was determined in Vero cells culture and fetal calf serum
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[PMID: 11300872] |
Olpadronic acid (5 × 10-8-10-4 M) potently inhibits bone resorption in foetal mouse bone assays with a CI50 of 5 × 10-7 M[1].
Olpadronic acid inhibits breast cancer cell adhesion to bone matrices[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Olpadronate maintains and restores mechanical bone quality in rats with immobilisation- or ovariectomy-induced osteopaenia[1].
Olpadronate (90 mg/kg/day; p.o.; long-term) improves the biomechanical strength of long bones in normal mice without impairing bone mineralisation[1].
Olpadronate enhances the anabolic bone effects of simultaneous hPTH administration in normal rats by inhibiting remodelling of newly formed bone[1].
Olpadronic acid (4-16 ug/100g; i.p.; once weekly; 30 days) prevents Cyclosporine-induced high bone resorption and trabecular bone loss in male Sprague-Dawley rats[2].
Olpadronate (2.6 mmol/L; i.v.; 3 doses total) prevents bone destruction and tumor growth in the skeletal prostate cancer mouse model[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Mice[1]
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Dosage:90 mg/kg/day
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Administration:p.o.; long-term
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Result:Improved the resistance of long bones to deformation and fracture.
Increased external diameter and diaphyseal moments of inertia for flexion and torsion.
Did not impair matrix calcification.
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Animal Model:Sprague-Dawley rats (male, ~5 months old, 250-300 g, cyclosporine-induced osteopenia)[2]
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Dosage:4; 8; 16 ug/100g rat
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Administration:i.p.; once weekly; 30 days
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Result:Caused a transient, statistically significant increase in serum bone-alkaline phosphatase (b-ALP) on day 14 in groups receiving 8 ug/100g and 16 ug/100g, and a significant reduction in serum b-ALP on day 30 compared to control and cyclosporine-only groups.
Significantly reduced urinary deoxypyridinoline (DPyr) excretion on days 14 and 30 compared to cyclosporine-only rats, with the 16 ug/100g dose causing a greater reduction than the lower doses.
Significantly increased BMD in the total skeleton, whole femur, lumbar spine, and proximal tibia on day 30 compared to control and cyclosporine-only rats.
Resulted in significantly higher proximal tibia, whole femur, and lumbar spine BMD with the 16 ug/100g dose compared to the lower olpadronic acid doses.
Showed no significant effects on middle tibia BMD with any dose.
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Animal Model:NCR nude (nu/nu) mice (6-month-old male, immunocompromised, intratibial inoculation with PC-3-GFP human prostate cancer cells)[3]
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Dosage:2.6 mmol/L
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Administration:i.v.; 3 times total (1 month pre-implantation, at implantation, and 30 days post-implantation)
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Result:Prevented tumor volume from exceeding 1 cm3.
Reduced GFP tumor area by 66% compared to tumor-bearing control mice.
Reduced mean X-ray score to 0.9, with 8 of 19 mice showing no tibial abnormalities and 11 showing only minor abnormalities, representing a dramatic reduction in bone lesion severity that was significantly greater than that seen with pamidronate.
Reduced serum calcium to 10.7 mg/dL compared to tumor-bearing control mice.
Reduced serum parathyroid hormone-related protein (PTHrP) to 110 pg/mL compared to tumor-bearing control mice.
Reduced serum osteoprotegerin to 58 pg/mL compared to tumor-bearing control mice.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 63132-39-8
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Appearance Solid
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Masse moléculaire 263.12
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Formule C5H15NO7P2
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Color White to off-white
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SMILES
O=P(O)(C(CCN(C)C)(P(O)(O)=O)O)O
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Synonyms
Olpadronate; OLP
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
H2O : 50 mg/mL (190.03 mM; Need ultrasonic and warming)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureté et documentation
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Fiche technique (280 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Roldán EJ, et al Olpadronate: a new amino-bisphosphonate for the treatment of medical osteopathies. Expert Opin Investig Drugs. 1998 Sep;7(9):1521-38. [Content Brief]
[2]. Zeni SN, et al. Olpadronate prevents the bone loss induced by cyclosporine in the rat. Calcif Tissue Int. 2002 Jan;70(1):48-53. [Content Brief]
[3]. Yang M, et al. The bisphosphonate olpadronate inhibits skeletal prostate cancer progression in a green fluorescent protein nude mouse model. Clin Cancer Res. 2006 Apr 15;12(8):2602-6. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| H2O | 1 mM | 3.8005 mL | 19.0027 mL | 38.0055 mL | 95.0137 mL |
| 5 mM | 0.7601 mL | 3.8005 mL | 7.6011 mL | 19.0027 mL | |
| 10 mM | 0.3801 mL | 1.9003 mL | 3.8005 mL | 9.5014 mL | |
| 15 mM | 0.2534 mL | 1.2668 mL | 2.5337 mL | 6.3342 mL | |
| 20 mM | 0.1900 mL | 0.9501 mL | 1.9003 mL | 4.7507 mL | |
| 25 mM | 0.1520 mL | 0.7601 mL | 1.5202 mL | 3.8005 mL | |
| 30 mM | 0.1267 mL | 0.6334 mL | 1.2668 mL | 3.1671 mL | |
| 40 mM | 0.0950 mL | 0.4751 mL | 0.9501 mL | 2.3753 mL | |
| 50 mM | 0.0760 mL | 0.3801 mL | 0.7601 mL | 1.9003 mL | |
| 60 mM | 0.0633 mL | 0.3167 mL | 0.6334 mL | 1.5836 mL | |
| 80 mM | 0.0475 mL | 0.2375 mL | 0.4751 mL | 1.1877 mL | |
| 100 mM | 0.0380 mL | 0.1900 mL | 0.3801 mL | 0.9501 mL |
Olpadronic acid Related Classifications
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