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Purity: ≥98%
Alfacalcidol (1-hydroxycholecalciferol), a potent and non-selective VDR activator drug, is an active metabolite of vitamin D that is frequently used to treat osteoporosis. Alfacalcidol has been shown to contribute to the homeostasis of bone and minerals by binding to the vitamin D receptor (VDR) in target organs related to calcium, including the kidney, parathyroid gland, intestine, and bone. Furthermore, it has been reported that Alfacalcidol, at pharmacological doses that do not result in hypercalcemia, inhibits osteoclastic bone resorption in a high bone-turnover state following OVX. Aside from this, alfacalcidol has demonstrated a stimulatory effect on the growth of new bone. Additionally, in the OVX model, alfacalcidol has been shown to increase bone mass and bone strength at specific serum and urinary calcium levels.
| ln Vivo |
The effects of ethanol are at least partially independent of calcium action. Alfacalcidol (0.025-0.1 mg/kg; channel; 5 times weekly; for 3 months) boosts vitamin D in this aspect and has bone preventive effects.
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| Animal Protocol |
Animal/Disease Models: Female Wistar-Imamichi rat (8 months old), ovariectomized [3]
Doses: 0.025mg/kg, 0.05mg/kg, 0.1mg/kg Route of Administration: oral; Inhibition of PTH[3]. Five times a week; lasted for 3 months. Experimental Results: exerted bone protective effects, independent of calcium-related effects. |
| References |
[1]. Galeşanu C, et al. [Postmenopausal osteoporosis. Digital Rx radiogrammetry in the diagnosis and follow-up of treatment with alfacalcidol]. Rev Med Chir Soc Med Nat Iasi. 2006 Oct-Dec;110(4):833-41.
[2]. Nuijten M, et al. Cost Effectiveness of Paricalcitol versus a Non-Selective Vitamin D Receptor Activator for Secondary Hyperparathyroidism in the UK. Clin Drug Investig. 2010;30(8):545-57. [3]. Shiraishi A, et al. The advantage of alfacalcidol over vitamin D in the treatment of osteoporosis. Calcif Tissue Int. 1999 Oct;65(4):311-6. [4]. Nagaoka H, et al. Alfacalcidol enhances collagen quality in ovariectomized rat bones. J Orthop Res. 2014 Aug;32(8):1030-6. |
| Molecular Formula |
C27H44O2
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| Molecular Weight |
400.64
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| Exact Mass |
400.33
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| Elemental Analysis |
C, 80.94; H, 11.07; O, 7.99
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| CAS # |
41294-56-8
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| Related CAS # |
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| Appearance |
Solid powder
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| SMILES |
C[C@H](CCCC(C)C)[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
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| InChi Key |
OFHCOWSQAMBJIW-AVJTYSNKSA-N
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| InChi Code |
InChI=1S/C27H44O2/c1-18(2)8-6-9-19(3)24-13-14-25-21(10-7-15-27(24,25)5)11-12-22-16-23(28)17-26(29)20(22)4/h11-12,18-19,23-26,28-29H,4,6-10,13-17H2,1-3,5H3/b21-11+,22-12-/t19-,23-,24-,25+,26+,27-/m1/s1
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| Chemical Name |
(1R,3S,5Z)-5-[(2E)-2-[(1R,3aS,7aR)-7a-methyl-1-[(2R)-6-methylheptan-2-yl]-2,3,3a,5,6,7-hexahydro-1H-inden-4-ylidene]ethylidene]-4-methylidenecyclohexane-1,3-diol
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| Synonyms |
Alfacalcidol; Alfarol; alpha-Calcidol; Alpha D 3; Bondiol; EB 644; Alpha-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 |
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| 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) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.24 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 25.0 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: 2.5 mg/mL (6.24 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 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: ≥ 2.5 mg/mL (6.24 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 | 2.4960 mL | 12.4800 mL | 24.9601 mL | |
| 5 mM | 0.4992 mL | 2.4960 mL | 4.9920 mL | |
| 10 mM | 0.2496 mL | 1.2480 mL | 2.4960 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 |
| NCT03210688 | Recruiting | Drug: Prednisolone Drug: Alfacalcidol |
Minimal Change Disease Nephrotic Syndrome |
University of Aarhus | May 1, 2018 | Phase 4 |
| NCT06016400 | Recruiting | Drug: Alfacalcidol Oral Solution Drug: Placebo |
Oral Mucositis Oral Squamous Cell Carcinoma |
Sun Yat-Sen Memorial Hospital of Sun Yat-Sen University |
June 14, 2021 | Phase 2 Phase 3 |
| NCT03582917 | Recruiting | Drug: Alphacalcidol | Scoliosis; Adolescence | University of Ioannina | September 20, 2018 | Phase 2 |
| NCT04967469 | Recruiting | Drug: Calcitriol Drug: Alfacalcidol 0.5 MCG Oral Capsule |
End Stage Renal Disease | Rajavithi Hospital | September 1, 2020 | Not Applicable |
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