Size | Price | Stock | Qty |
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10mg |
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25mg |
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50mg |
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100mg |
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Other Sizes |
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Purity: ≥98%
Tiludronate (Tiludronate disodium; Tiludronic Acid disodium) is a novel and potent bisphosphonate agent which prevents postmenopausal bone loss and is used for treatment of Paget's disease of bone (osteitis deformans) in human medicine. In veterinary medicine, tiludronic acid is used to treat navicular disease and bone spavin in horses. Its trade names are Tildren and Equidronate. It is approved for treatment of navicular disease and distal tarsal osteoarthritis in Europe, and was approved for treatment of navicular disease in the United States in 2014. Tiludronate is a non-nitrogenous bisphosphonate that inhibits osteoclasts, the primary cell responsible for the breakdown of bone required for bone remodeling.
ln Vitro |
The inhibition of proton transport by tiludronate is 5-fold greater in nephrogenic vesicles (IC50=1.1 mM) and 10,000-fold more in vesicles produced from osteoclasts (IC50=466 nM). Additionally, tiludronate efficiently suppresses the activity of pure yeast V-ATPase and inhibits proton transport in yeast microsomal preparations (IC50=3.5 microM). Tiludronate quickly and reversibly inhibits the proton transport process mediated by osteoclast V-ATPase, subject to pH variations [3].
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ln Vivo |
Tiludronate inhibits bone resorption in a dose-dependent manner. Mature osteoclasts can be affected by tiludronate by decreased proton secretion into the resorption space and increased osteoclast dissociation from the bone matrix. Several models of osteoporosis have also been used to test teludronate. Tiladronate sodium (5–200 mg/kg; oral) reduced the loss of bone mass in a male ovariectomized rat model. This was measured chemically by evaluating the calcium and phosphate content or physically by assessing bone weight and density[3].
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References |
[1]. Reginster JY, et al. Prevention of postmenopausal bone loss by tiludronate. Lancet. 1989 Dec 23-30;2(8678-8679):1469-71.
[2]. Nunes NLT, et al. Effects of local administration of tiludronic acid on experimental periodontitis in diabetic rats. J Periodontol. 2018 Jan;89(1):105-116. [3]. Bonjour JP, et al. Tiludronate: bone pharmacology and safety. Bone. 1995;17(5 Suppl):473S-477S. [4]. David P, et al. The bisphosphonate tiludronate is a potent inhibitor of the osteoclast vacuolar H(+)-ATPase. J Bone Miner Res. 1996;11(10):1498-1507. |
Molecular Formula |
C7H7CLNA2O6P2S
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Molecular Weight |
362.5719
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CAS # |
149845-07-8
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Related CAS # |
Tiludronate;89987-06-4;Tiludronate-d5 sodium
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
O=P(O)(C(SC1=CC=C(Cl)C=C1)P([O-])(O)=O)[O-].[Na+].[Na+]
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InChi Key |
SKUHWSDHMJMHIW-UHFFFAOYSA-L
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InChi Code |
InChI=1S/C7H9ClO6P2S.2Na/c8-5-1-3-6(4-2-5)17-7(15(9,10)11)16(12,13)14/h1-4,7H,(H2,9,10,11)(H2,12,13,14)/q2*+1/p-2
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Chemical Name |
[(4-chlorophenyl)sulfanyl-[hydroxy(oxido)phosphoryl]methyl]-hydroxyphosphinate disodium
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Synonyms |
Tiludronate disodium Tiludronic Acid disodium Tiludronic acid Skelid Tildren Equidronate.
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
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 : ~62.5 mg/mL (~172.38 mM)
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Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.7581 mL | 13.7904 mL | 27.5809 mL | |
5 mM | 0.5516 mL | 2.7581 mL | 5.5162 mL | |
10 mM | 0.2758 mL | 1.3790 mL | 2.7581 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.