| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| Other Sizes |
| Targets |
Maxacalcitol-D6 is the deuterated form of maxacalcitol, which targets the vitamin D receptor (VDR). Maxacalcitol binds VDR with high affinity and activates VDR-mediated gene transcription. It suppresses PTH synthesis and secretion. It has a non-calcemic profile, meaning it has less effect on serum calcium than calcitriol. It is a VDR ligand with therapeutic potential for secondary hyperparathyroidism and psoriasis.
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|---|---|
| ln Vitro |
In vitro, maxacalcitol (the unlabeled parent) suppresses PTH mRNA expression in parathyroid cells. It exhibits similar effects to calcitriol in osteoblast-like cells, including induction of osteocalcin and alkaline phosphatase. It inhibits the growth of osteosarcoma cells in vitro in combination with all-trans retinoic acid. The deuterated form has equivalent biological activity.
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| ln Vivo |
In vivo, maxacalcitol (22-oxacalcitriol) suppresses secondary hyperparathyroidism without inducing low bone turnover in dogs with renal failure. It inhibits tumor growth of osteosarcoma in vivo and its pulmonary metastasis. It has a longer half-life than calcitriol. It is used clinically in Japan for secondary hyperparathyroidism and psoriasis. The deuterated form is used as an internal standard for pharmacokinetic studies.
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| Enzyme Assay |
For non-cell receptor binding assays, recombinant VDR ligand-binding domain is incubated with radiolabeled calcitriol and Maxacalcitol-D6 at serial dilutions. Bound radioligand is separated by charcoal adsorption or filtration. IC50 values are calculated from competition curves. VDR-mediated transcription is measured by luciferase reporter assay using purified VDR and coactivators.
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| Cell Assay |
In cell assays, osteoblast-like cells or parathyroid cells are treated with Maxacalcitol-D6. PTH mRNA expression is measured by qPCR. Osteocalcin and alkaline phosphatase expression are measured by ELISA or qPCR. Cell proliferation is measured by MTT. VDR target gene expression (e.g., CYP24A1) is measured by qPCR.
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| Animal Protocol |
In vivo animal protocols use dogs with renal failure or rats with secondary hyperparathyroidism. Maxacalcitol-D6 is administered intravenously or orally. Serum PTH, calcium, and phosphorus levels are measured. Bone histomorphometry is assessed. Pharmacokinetic parameters are determined by LC-MS/MS. The deuterated form is used as an internal standard.
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| References |
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| Molecular Formula |
C26H42O4
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|---|---|
| Molecular Weight |
424.65
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| Exact Mass |
424.34597029
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| Related CAS # |
Maxacalcitol; 103909-75-7
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| Appearance |
White to off-white solid
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| SMILES |
O[C@@H](C[C@H](O)C/1=C)CC1=C\C=C2[C@@](CC[C@@H]3[C@@H](OCCC(C([2H])([2H])[2H])(C([2H])([2H])[2H])O)C)([H])[C@]3(C)CCC\2
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| InChi Key |
DTXXSJZBSTYZKE-OXMAATCFSA-N
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| InChi Code |
InChI=1S/C26H42O4/c1-17-20(15-21(27)16-24(17)28)9-8-19-7-6-12-26(5)22(10-11-23(19)26)18(2)30-14-13-25(3,4)29/h8-9,18,21-24,27-29H,1,6-7,10-16H2,2-5H3/b19-8+,20-9-/t18-,21+,22+,23-,24-,26+/m0/s1/i3D3,4D3
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| Chemical Name |
(1R,3S,5Z)-5-[(2E)-2-[(1S,3aS,7aS)-7a-methyl-1-[(1S)-1-[4,4,4-trideuterio-3-hydroxy-3-(trideuteriomethyl)butoxy]ethyl]-2,3,3a,5,6,7-hexahydro-1H-inden-4-ylidene]ethylidene]-4-methylidenecyclohexane-1,3-diol
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| Synonyms |
Maxacalcitol-D6
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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: (1). This product requires protection from light (avoid light exposure) during transportation and storage. (2). Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. (3). This product is not stable in solution, please use freshly prepared working solution for optimal results. |
| 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: ~100 mg/mL (~235.5 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.89 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), Clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.89 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), Clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 900 μL of 20% SBE-β-CD saline and mix well. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 3: ≥ 2.5 mg/mL (5.89 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), Clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 900 μL of corn oil and mix well. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3549 mL | 11.7744 mL | 23.5488 mL | |
| 5 mM | 0.4710 mL | 2.3549 mL | 4.7098 mL | |
| 10 mM | 0.2355 mL | 1.1774 mL | 2.3549 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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