| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 25mg |
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| 50mg | |||
| Other Sizes |
Purity: ≥98%
| Targets |
Maxacalcitol targets the vitamin D receptor (VDR), a nuclear receptor that regulates gene transcription. It is a VDR-like receptor ligand. Activation of VDR leads to modulation of gene expression involved in cell proliferation, differentiation, and immune function. The compound suppresses parathyroid hormone (PTH) mRNA expression.
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| ln Vitro |
Maxacalcitol inhibits parathyroid hormone (PTH) mRNA expression in vitro. It exhibits similar effects to calcitriol in osteoblast-like cells. The compound inhibits tumor growth of osteosarcoma in vitro when combined with all-trans retinoic acid. These activities confirm VDR-mediated transcriptional regulation.
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| ln Vivo |
Maxacalcitol inhibits parathyroid hormone (PTH) mRNA expression in vivo. It suppresses secondary hyperparathyroidism without inducing low bone turnover in dogs with renal failure. The compound also inhibits tumor growth of a canine osteosarcoma cell line in vivo and prevents pulmonary metastasis. These activities support its therapeutic potential.
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| Enzyme Assay |
Non-cell-based receptor binding assays for Maxacalcitol typically use purified VDR protein or VDR-containing nuclear extracts. The compound is incubated with radiolabeled calcitriol or other VDR ligands in competitive binding assays. Binding affinity (Ki) is determined by measuring displacement of the radiolabeled ligand. Assays are performed in buffer systems with appropriate salt concentrations and incubation times, followed by separation of bound from free ligand.
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| Cell Assay |
Cellular assays for Maxacalcitol utilize VDR-expressing cell lines such as osteoblast-like cells, keratinocytes, or cancer cells. Cells are treated with the compound at various concentrations, and gene expression changes are measured by quantitative PCR for VDR target genes (e.g., CYP24A1, osteocalcin). PTH mRNA expression is assessed in parathyroid cells. Cell proliferation and differentiation are measured using standard assays.
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| Animal Protocol |
In vivo animal models for Maxacalcitol include renal failure models in dogs to assess suppression of secondary hyperparathyroidism, osteosarcoma xenograft models to evaluate antitumor activity, and models of psoriasis. The compound is administered orally at various doses. Efficacy is assessed through serum PTH levels, bone turnover markers, tumor growth measurements, and histopathological analysis.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of Maxacalcitol include molecular weight of 418.61 g/mol and molecular formula C26H42O4. The compound is soluble in DMSO (100 mg/mL). As an orally active vitamin D analog, it is designed for oral administration. Storage: powder at -20°C for 3 years; in solvent at -80°C for 1 year.
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| Toxicity/Toxicokinetics |
Maxacalcitol is a non-calcemic vitamin D3 analog with limited calcemic effect, meaning it has reduced potential to cause hypercalcemia compared to calcitriol. This improved safety profile makes it suitable for chronic use. Standard toxicity assessments would evaluate effects on calcium metabolism, renal function, and bone turnover. The compound is approved for psoriasis.
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| References |
[4]. Successful Treatment of Bowen's Disease with Topical Maxacalcitol.Acta Derm Venereol. 2012 Jan 26. [5]. Effects of maxacalcitol ointment on skin lesions in patients with psoriasis receiving treatment with adalimumab. J Dermatol. 2016 Nov;43(11):1354-1357. doi: 10.1111/1346-8138.13515. Epub 2016 Jul 23. PubMed PMID: 27450634. |
| Additional Infomation |
Maxacalcitol is an organic molecular entity.
Maxacalcitol is also known as 22-Oxacalcitriol, OCT, Sch-209579, MC-1275, Oxarol, and Prezios. It has CAS number 103909-75-7. The compound is used clinically as an antipsoriatic agent and is also studied for treatment of hyperparathyroidism. It has cardioprotective effects in diabetes mellitus and induces hCAP-18/LL-37 production in human oral epithelial cells. |
| Molecular Formula |
C26H42O4
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|---|---|
| Molecular Weight |
418.61
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| Exact Mass |
418.308
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| Elemental Analysis |
C, 74.60; H, 10.11; O, 15.29
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| CAS # |
103909-75-7
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| Related CAS # |
103909-75-7
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| PubChem CID |
6398761
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| Appearance |
White to off-white solid powder
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| Density |
1.1±0.1 g/cm3
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| Boiling Point |
581.4±50.0 °C at 760 mmHg
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| Flash Point |
305.4±30.1 °C
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| Vapour Pressure |
0.0±3.7 mmHg at 25°C
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| Index of Refraction |
1.549
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| LogP |
4.38
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
30
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| Complexity |
691
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| Defined Atom Stereocenter Count |
6
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| SMILES |
C[C@@H]([C@H]1CC[C@@H]\2[C@@]1(CCC/C2=C\C=C/3\C[C@H](C[C@@H](C3=C)O)O)C)OCCC(C)(C)O
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| InChi Key |
DTXXSJZBSTYZKE-ZDQKKZTESA-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
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| Chemical Name |
(1R,3S,5Z)-5-[(2E)-2-[(1S,3aS,7aS)-1-[(1S)-1-(3-hydroxy-3-methylbutoxy)ethyl]-7a-methyl-2,3,3a,5,6,7-hexahydro-1H-inden-4-ylidene]ethylidene]-4-methylidenecyclohexane-1,3-diol
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| Synonyms |
OCT; Maxacalcitol; Maxacalcitriol; MC 1275; Prezios; 22-Oxacalcitriol; Sch 209579; 22-Oxa-1,25-dihydroxyvitamin D3; alpha,25-Dihydroxy-22-oxavitamin D3
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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: ~50 mg/mL (~119.4 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.67 mg/mL (3.99 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 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 16.7 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to 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: ≥ 1.67 mg/mL (3.99 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 16.7 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. 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. View More
Solubility in Formulation 3: ≥ 1.67 mg/mL (3.99 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3889 mL | 11.9443 mL | 23.8886 mL | |
| 5 mM | 0.4778 mL | 2.3889 mL | 4.7777 mL | |
| 10 mM | 0.2389 mL | 1.1944 mL | 2.3889 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 |
| NCT01341782 | Completed | Drug: maxacalcitol Drug: paricalcitol |
Secondary Hyperparathyroidism Hemodialysis |
AbbVie (prior sponsor, Abbott) |
May 2011 | Phase 3 |
| NCT00990704 | Completed | Drug: paricalcitol Drug: maxacalcitol |
Secondary Hyperparathyroidism Hemodialysis |
Abbott | October 2009 | Phase 2 |
| NCT00667576 | Completed | Drug: paricalcitol Drug: Maxacalcitol |
Chronic Kidney Disease on Hemodialysis Secondary Hyperparathyroidism |
Abbott | April 2008 | Phase 2 |
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