| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| Other Sizes |
| Targets |
Vitamin D receptor (VDR); functions as an agonist, binding to VDR in bone and intestine to regulate calcium and phosphate homeostasis and bone mineralization.
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|---|---|
| ln Vitro |
Eldecalcitol can greatly enhance bone density and has a strong inhibitory effect on bone resorption [1].
Unlabeled Eldecalcitol possesses a strong inhibitory effect on bone resorption (via suppression of osteoclast activity) and causes a significant increase in bone mineral density in osteoblast cultures. It enhances osteocalcin levels in osteoblasts. |
| ln Vivo |
In preclinical animal models, Eldecalcitol (orally administered at 0.1-0.5 microg/kg daily) increases bone mineral density, improves bone microarchitecture, and reduces fracture risk. In postmenopausal osteoporotic patients, Eldecalcitol significantly increases lumbar spine BMD.
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| Enzyme Assay |
VDR binding affinity is assessed by competitive radioligand binding assays using [3H]-1,25-dihydroxyvitamin D3 and recombinant VDR protein; unlabeled Eldecalcitol competes for binding, and the d6-labeled compound is used as an internal standard in quantification.
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| Cell Assay |
Osteoblasts (e.g., MC3T3-E1) or osteoclast precursors are treated with Eldecalcitol-d6 as internal standard; unlabeled Eldecalcitol (0.1-100 nM) is added; osteocalcin expression is measured by qPCR or ELISA; osteoclast differentiation is assessed by TRAP staining.
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| Animal Protocol |
Rats or mice are orally administered Eldecalcitol-d6 as an internal standard; plasma and bone tissue samples are collected at various time points; samples are extracted and analyzed by LC-MS/MS to quantify unlabeled Eldecalcitol concentrations.
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| ADME/Pharmacokinetics |
Identical to unlabeled Eldecalcitol; orally bioavailable with a long half-life (approximately 24 hours in humans); highly protein-bound (99.8%); metabolized primarily in the liver via CYP24A1; the d6 label does not alter PK properties.
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| Toxicity/Toxicokinetics |
No toxicity data for the d6 analog; Eldecalcitol has a favorable safety profile in clinical use; common adverse effects include mild hypercalcemia, nausea, and gastrointestinal discomfort; long-term safety established in osteoporosis patients.
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| References |
[1]. Noguchi Y, et al. Eldecalcitol for the treatment of osteoporosis. Clin Interv Aging. 2013;8:1313-21.
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| Additional Infomation |
Eldecalcitol (ED-71, brand name Edirol) is approved in Japan for the treatment of osteoporosis. The d6-labeled version is a research-grade analytical standard for LC-MS/MS quantification.
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| Molecular Formula |
C30H44D6O5
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|---|---|
| Molecular Weight |
496.75
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| Related CAS # |
Eldecalcitol;104121-92-8
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| Appearance |
Typically exists as solid at room temperature
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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) |
DMSO :~25 mg/mL (~50.33 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 | 2.0131 mL | 10.0654 mL | 20.1309 mL | |
| 5 mM | 0.4026 mL | 2.0131 mL | 4.0262 mL | |
| 10 mM | 0.2013 mL | 1.0065 mL | 2.0131 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.
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