Identification
- Summary
Alfacalcidol is a vitamin D analogue used for the management of hypocalcemia, secondary hyperparathyroidism, and osteodystrophy in patients with chronic renal failure, as well as some types of rickets and osteomalacia.
- Brand Names
- One-alpha
- Generic Name
- Alfacalcidol
- DrugBank Accession Number
- DB01436
- Background
Alfacalcidol, or 1-alpha-hydroxycholecalciferol or 1-alpha-hydroxyvitamin D3, is a non-endogenous analogue of vitamin D.4 It plays an essential function in calcium homeostasis and bone metabolism. Alfacaldisol is activated by the enzyme 25-hydroxylase in the liver to mediate its effects in the body, or most importantly, the kidneys and bones. The pharmacological actions of alfacalcidol are prolonged than vitamin D because a negative feedback mechanism regulates the final activation step of vitamin D in the kidneys.1,2
Alfacalcidol is available in oral and intravenous formulations. In Canada, it is marketed as ONE-ALPHA, which manages hypocalcemia, secondary hyperparathyroidism, and osteodystrophy in adults with chronic renal failure.9 In approving European countries, alfacalcidol is also indicated for managing nutritional and malabsorptive rickets and osteomalacia, vitamin D-dependent rickets and osteomalacia, and hypophosphataemic vitamin D resistant rickets and osteomalacia.11,12
- Type
- Small Molecule
- Groups
- Approved, Nutraceutical
- Structure
Structure for Alfacalcidol (DB01436)
- Weight
- Average: 400.6371
Monoisotopic: 400.334130652 - Chemical Formula
- C27H44O2
- Synonyms
- (5Z,7E)-9,10-seco-5,7,10(19)-cholestatrien-1α,3β-diol
- 1-hydroxycholecalciferol
- 1alpha-hydroxycholecalciferol
- 1α-hydroxy-vitamin D3
- 1α-hydroxycholecalciferol
- 1α-hydroxyvitamin D3
- 9,10-secocholesta-5,7,10(19)-triene-1α,3β-diol
- Alfacalcidol
- Alfacalcidolum
Pharmacology
- Indication
Alfacalcidol is indicated in adult patients with chronic renal failure for the management of hypocalcemia, secondary hyperparathyroidism, or osteodystrophy.9
Alfacalcidol is indicated in the management of nutritional and malabsorptive rickets and osteomalacia, vitamin D-dependent rickets and osteomalacia, and hypophosphataemic vitamin D resistant rickets and osteomalacia.11,12
Reduce drug development failure ratesBuild, train, & validate machine-learning modelswith evidence-based and structured datasets.Build, train, & validate predictive machine-learning models with structured datasets.- Associated Conditions
Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Management of Hypocalcemia •••••••••••• ••••• Management of Hypophosphatemic rickets •••••••••••• ••••••• Management of Hypovitaminosis d •••••••••••• ••••••• Management of Hypovitaminosis d •••••••••••• ••••••• Management of Nutritional rickets •••••••••••• ••••••• - Contraindications & Blackbox Warnings
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Alfacalcidol works to increase serum levels of calcium by stimulating intestinal calcium absorption, reabsorption of calcium from bone, and possibly the renal reabsorption of calcium. It also modestly promotes intestinal phosphorus absorption.9 In patients with renal failure, alfacalcidol increased intestinal calcium and phosphorus absorption in a dose-related manner. This increase in calcium and phosphorus levels occurs within three days following drug administration: this effect was reversed within three days of drug discontinuation. In patients with chronic renal failure, serum calcium levels were elevated while parathyroid hormone and alkaline phosphatase levels returned to normal levels within five days following alfacalcidol administration.12 Since alfacalcidol suppresses parathyroid hormone, a reduction in parathyroid hormone levels is achieved more rapidly in patients on intermittent intravenous therapy, with significant reductions occurring within three months of therapy. In patients receiving daily oral therapy of alfacalcidol, the time it takes alfacalcidol to normalize plasma calcium levels may be up to several months, possibly reflecting calcium being utilized for bone mineralization.9 In patients with nutritional osteomalacia, alfacalcidol increased calcium absorption with six hours of oral administration and the effects peaked at 24 hours.12
- Mechanism of action
In conditions like chronic renal failure, renal bone disease, hypoparathyroidism, and vitamin D dependent rickets, the kidneys' capacity for 1α-hydroxylation is impaired, leading to reduced production of endogenous 1,25-dihydroxyvitamin D and aberrated mineral metabolism. As an active and potent analog of vitamin D, alfacalcidol works to restore the functions and activities of endogenous 1,25-dihydroxyvitamin D.12
Target Actions Organism AVitamin D3 receptor agonistHumans U25-hydroxyvitamin D-1 alpha hydroxylase, mitochondrial Not Available Humans URetinoic acid receptor RXR-alpha Not Available Humans - Absorption
Alfacalcidol is absorbed passively and almost completely in the small intestine.12
- Volume of distribution
Not Available
- Protein binding
The active metabolite of alfacalcidol, 1,25-dihydroxyvitamin D, is transported to tissues via globulin, a specific transport protein.12
- Metabolism
Alfacalcidol is rapidly converted in the liver to 1,25-dihydroxyvitamin D, which is essentially the metabolite of vitamin D that regulates calcium and phosphate metabolism. Alfacalcidol is further metabolized to other polar inactive metabolites, excreted primarily through the bile.12
- Route of elimination
Not Available
- Half-life
The half-life of alfacalcidol ranges from three to four hours.9,12
- Clearance
Not Available
- Adverse Effects
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There is a discrepancy across a number of reported LD50 values for alfacalcidol, which can be attributed to differences in the procedures used in laboratories. Oral LD50 in mice ranges from 440 to 490 mcg/kg. Intravenous in mice was 290 mcg/kg; however, another source presented 56 mcg/kg in female mice and 71 mcg/kg in male mice. Oral LD50 in rats ranges from 340 to 720 mcg/kg.9
In case of an acute accidental overdose following oral administration, emesis or gastric lavage can be induced to prevent further drug absorption. Mineral oil may be used to promote fecal drug elimination in instances where the drug was already absorbed in the stomach.9
Alfacalcidol overdose can lead to hypercalcemia, hypercalciuria, and hyperphosphatemia. Similarly, a high intake of calcium and phosphate concurrently with a therapeutic dose of alfacalcidol can result in those conditions.9 Hypercalcemia most commonly presents with headache, weakness, hypertension, somnolence, dizziness, sweating, anorexia, nausea, vomiting, diarrhea, constipation, polyuria, polydipsia and muscle and bone pain, and metallic taste.12 Hypercalcemia should be responded to with discontinuation of alfacalcidol, a low calcium diet and withdrawal of calcium supplements.9 Prolonged hypercalcemia can lead to nephrocalcinosis, nephrolithiasis, and reduced kidney function. In cases of severe hypercalcemia, general supportive measures are recommended, which may include forced diuresis and close monitoring of renal function, electrolytes, and electrocardiographs. Monitoring for abnormalities is especially critical in patients receiving digitalis glycosides. Management with glucocorticosteroids, loop diuretics, bisphosphonates, and calcitonin, as well as hemodialysis with low calcium content, may be considered.12
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs Browse all" title="About SNP Mediated Effects/ADRs" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">
- Not Available
Interactions
- Drug Interactions Learn More" title="About Drug Interactions" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Integrate drug-drug
interactions in your softwareAcetyldigitoxin The risk or severity of ventricular arrhythmias and Cardiac Arrhythmia can be increased when Alfacalcidol is combined with Acetyldigitoxin. Aluminum hydroxide The serum concentration of Aluminum hydroxide can be increased when it is combined with Alfacalcidol. Beclomethasone dipropionate The therapeutic efficacy of Alfacalcidol can be decreased when used in combination with Beclomethasone dipropionate. Bendroflumethiazide The risk or severity of hypercalcemia can be increased when Bendroflumethiazide is combined with Alfacalcidol. Benzthiazide The risk or severity of hypercalcemia can be increased when Benzthiazide is combined with Alfacalcidol. - Food Interactions
- Take with or without food. Food does not affect the bioavailability.
Products
Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.- International/Other Brands
- Alsiodol / One Alpha
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Alfacalcidol Capsules Capsule 0.25 mcg Oral Strides Pharma Canada Inc Not applicable Not applicable Canada 
Alfacalcidol Capsules Capsule 1 mcg Oral Strides Pharma Canada Inc Not applicable Not applicable Canada One-alpha Capsule 0.25 mcg Oral Cheplapharm Arzneimittel Gmbh 1980-12-31 Not applicable Canada One-alpha Solution 2 mcg / mL Intravenous Cheplapharm Arzneimittel Gmbh 2001-02-20 Not applicable Canada One-alpha Capsule 1 mcg Oral Cheplapharm Arzneimittel Gmbh 1980-12-31 Not applicable Canada - Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Sandoz Alfacalcidol Capsule 1 mcg Oral Sandoz Canada Incorporated 2023-04-24 Not applicable Canada Sandoz Alfacalcidol Capsule 0.25 mcg Oral Sandoz Canada Incorporated 2023-04-24 Not applicable Canada - Over the Counter Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Alfa-D 0.25mcg Capsule Capsule Oral PAHANG PHARMACY SDN. BHD. 2020-09-08 Not applicable Malaysia 
Alfa-D 1.00mcg Capsule Capsule Oral PAHANG PHARMACY SDN. BHD. 2020-09-08 Not applicable Malaysia Alfacip 0.25mcg capsule Capsule Oral CIPLA MALAYSIA SDN BHD 2020-09-08 Not applicable Malaysia Alfacip 1mcg capsule Capsule 1 mcg Oral CIPLA MALAYSIA SDN BHD 2020-09-08 Not applicable Malaysia Alfost 0.25mcg (Alfacalcidol Capsule) Capsule 0.25 mcg Oral NVS REGULATORY SERVICES SDN BHD 2021-12-02 Not applicable Malaysia - Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image TEVABONE 70MG12TAB+1UG84KA Alfacalcidol (1 mcg) + Alendronic acid (70 mg) Tablet 2014-07-01 Not applicable Germany 
TEVABONE 70MG4TAB+1UG28KAP Alfacalcidol (1 mcg) + Alendronic acid (70 mg) Tablet 2014-07-01 Not applicable Germany
Categories
- ATC Codes
- A11CC03 — Alfacalcidol
- A11CC — Vitamin D and analogues
- A11C — VITAMIN A AND D, INCL. COMBINATIONS OF THE TWO
- A11 — VITAMINS
- A — ALIMENTARY TRACT AND METABOLISM
- Drug Categories
- Alimentary Tract and Metabolism
- Bone Density Conservation Agents
- Cholestanes
- Cholestenes
- Drugs Affecting Bone Structure and Mineralization
- Drugs for Treatment of Bone Diseases
- Fused-Ring Compounds
- Lipids
- Membrane Lipids
- Musculo-Skeletal System
- Secosteroids
- Steroids
- Sterols
- Vitamin D and Analogues
- Vitamins
- Vitamins (Fat Soluble)
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as vitamin d and derivatives. These are compounds containing a secosteroid backbone, usually secoergostane or secocholestane.
- Kingdom
- Organic compounds
- Super Class
- Lipids and lipid-like molecules
- Class
- Steroids and steroid derivatives
- Sub Class
- Vitamin D and derivatives
- Direct Parent
- Vitamin D and derivatives
- Alternative Parents
- Triterpenoids / Secondary alcohols / Cyclic alcohols and derivatives / Hydrocarbon derivatives
- Substituents
- Alcohol / Aliphatic homopolycyclic compound / Cyclic alcohol / Hydrocarbon derivative / Organic oxygen compound / Organooxygen compound / Secondary alcohol / Triterpenoid
- Molecular Framework
- Aliphatic homopolycyclic compounds
- External Descriptors
- diol, seco-cholestane, D3 vitamins, hydroxycalciol (CHEBI:31186) / Vitamin D3 and derivatives (LMST03020231)
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- URQ2517572
- CAS number
- 41294-56-8
- InChI Key
- OFHCOWSQAMBJIW-AVJTYSNKSA-N
- InChI
- 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
- IUPAC Name
- (1R,3S,5Z)-5-{2-[(1R,3aS,4E,7aR)-7a-methyl-1-[(2R)-6-methylheptan-2-yl]-octahydro-1H-inden-4-ylidene]ethylidene}-4-methylidenecyclohexane-1,3-diol
- SMILES
- CC(C)CCC[C@@H](C)[C@@]1([H])CC[C@@]2([H])\C(CCC[C@]12C)=C\C=C1\C[C@@H](O)C[C@H](O)C1=C
References
- General References
- Galesanu C, Ciubotariu C, Melnic G, Galesanu MR: [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. [Article]
- Ringe JD, Schacht E: Improving the outcome of established therapies for osteoporosis by adding the active D-hormone analog alfacalcidol. Rheumatol Int. 2007 Dec;28(2):103-11. doi: 10.1007/s00296-007-0422-6. Epub 2007 Aug 1. [Article]
- Vervloet M: Clinical uses of 1-alpha-hydroxycholecalciferol. Curr Vasc Pharmacol. 2014 Mar;12(2):300-5. doi: 10.2174/15701611113119990132. [Article]
- Richy F, Deroisy R, Lecart MP, Hanssens L, Mawet A, Reginster JY: D-hormone analog alfacalcidol: an update on its role in post-menopausal osteoporosis and rheumatoid arthritis management. Aging Clin Exp Res. 2005 Apr;17(2):133-42. doi: 10.1007/BF03324586. [Article]
- Shiraishi A, Takeda S, Masaki T, Higuchi Y, Uchiyama Y, Kubodera N, Sato K, Ikeda K, Nakamura T, Matsumoto T, Ogata E: Alfacalcidol inhibits bone resorption and stimulates formation in an ovariectomized rat model of osteoporosis: distinct actions from estrogen. J Bone Miner Res. 2000 Apr;15(4):770-9. doi: 10.1359/jbmr.2000.15.4.770. [Article]
- Shiraishi A, Higashi S, Ohkawa H, Kubodera N, Hirasawa T, Ezawa I, Ikeda K, Ogata E: The advantage of alfacalcidol over vitamin D in the treatment of osteoporosis. Calcif Tissue Int. 1999 Oct;65(4):311-6. doi: 10.1007/s002239900704. [Article]
- O'Donnell S, Moher D, Thomas K, Hanley DA, Cranney A: Systematic review of the benefits and harms of calcitriol and alfacalcidol for fractures and falls. J Bone Miner Metab. 2008;26(6):531-42. doi: 10.1007/s00774-008-0868-y. Epub 2008 Nov 1. [Article]
- Schacht E, Richy F, Reginster JY: The therapeutic effects of alfacalcidol on bone strength, muscle metabolism and prevention of falls and fractures. J Musculoskelet Neuronal Interact. 2005 Jul-Sep;5(3):273-84. [Article]
- LEO Pharma Inc. Product Monograph: ONE-ALPHA (alfacalcidol), for oral and intravenous use [Link]
- Biosynth Carbosynth: Alfacalcidol Safety Data Sheet [Link]
- AIFA Package Leaflet: DEDIOL (Alfacalcidol) for oral and intravenous use [Link]
- Summary of Product Characteristics: Alfacalcidol Aristo oral capsules [Link]
- External Links
- Human Metabolome Database
- HMDB0015504
- KEGG Drug
- D01518
- PubChem Compound
- 5282181
- PubChem Substance
- 46505115
- ChemSpider
- 4445376
- 12062
- ChEBI
- 31186
- ChEMBL
- CHEMBL1601669
- ZINC
- ZINC000012484965
- PharmGKB
- PA164746469
- PDBe Ligand
- M9B
- Wikipedia
- Alfacalcidol
- PDB Entries
- 6t0h
- FDA label
- Download (123 KB)
Clinical Trials
- Clinical Trials Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
Phase Status Purpose Conditions Count 4 Completed Prevention Cardiac Valve Replacement Complication 1 4 Completed Treatment End Stage Renal Disease (ESRD) / Secondary Hyperparathyroidism (SHPT) 1 4 Completed Treatment Fall / Osteopenia (Disorder) / Postmenopausal Osteoporosis 1 4 Completed Treatment Systemic Lupus Erythematosus 1 4 Completed Treatment Type 2 Diabetic Nephropathy 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Capsule Oral Solution / drops Oral Capsule Oral 0.25 UG Capsule Oral 0.5 UG Capsule Oral 1 UG Capsule Oral 1.0 UG Capsule Oral 1.0 mcg Capsule, liquid filled Oral 0.25 cg Capsule, liquid filled Oral 1 cg Tablet Oral Tablet Oral 0.25 mcg Tablet Oral 0.5 mcg Tablet Oral 1 MCG Solution / drops Oral 2 mcg/mL Solution / drops Oral 5 MCG/ML Solution Oral 2 UG/ML Capsule Oral 0.25 µg Injection, solution Intravenous 1 µg/0.5mL Capsule Oral 1.0 µg Injection, solution Intravenous 2 µg/mL Capsule Oral 1 MICROGRAMMI Solution / drops Oral 2 MICROGRAMMI/1ML Capsule, gelatin coated Oral Capsule Oral 1 mcg Capsule Oral 0.5 mcg Solution Intravenous 2 mcg / mL Solution / drops Oral 2 mcg / mL Capsule Oral 0.25 mcg Injection, solution Intravenous 1 mcg/0.5ml Injection, solution Intravenous 2 mcg/ml Capsule, liquid filled Oral 0.25 mcg Capsule, liquid filled Oral 1 mcg Capsule, liquid filled Oral 0.5 mcg Solution Oral 2 mcg/ml Injection Intravenous 2 mcg/ml Injection, solution Intravenous Liquid Oral .2 mcg / mL Capsule Oral 0.25 MICROGRAMMI Tablet - Prices
Unit description Cost Unit One-Alpha 2 mcg/ml 17.28USD ml One-Alpha 2 mcg/ml Drops 5.39USD ml One-Alpha 1 mcg Capsule 1.41USD capsule One-Alpha 0.25 mcg Capsule 0.47USD capsule DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
- Not Available
Properties
- State
- Solid
- Experimental Properties
Property Value Source melting point (°C) 136 °C PhysProp water solubility <1 mg/mL https://www.selleck.cn/msds/MSDS_S1468.pdf - Predicted Properties
Property Value Source Water Solubility 0.00163 mg/mL ALOGPS logP 6.68 ALOGPS logP 5.82 Chemaxon logS -5.4 ALOGPS pKa (Strongest Acidic) 14.39 Chemaxon pKa (Strongest Basic) -2.8 Chemaxon Physiological Charge 0 Chemaxon Hydrogen Acceptor Count 2 Chemaxon Hydrogen Donor Count 2 Chemaxon Polar Surface Area 40.46 Å2 Chemaxon Rotatable Bond Count 6 Chemaxon Refractivity 124.7 m3·mol-1 Chemaxon Polarizability 50.56 Å3 Chemaxon Number of Rings 3 Chemaxon Bioavailability 1 Chemaxon Rule of Five No Chemaxon Ghose Filter No Chemaxon Veber's Rule No Chemaxon MDDR-like Rule Yes Chemaxon - Predicted ADMET Features
Property Value Probability Human Intestinal Absorption + 0.9865 Blood Brain Barrier + 0.9142 Caco-2 permeable + 0.7866 P-glycoprotein substrate Substrate 0.7469 P-glycoprotein inhibitor I Non-inhibitor 0.5785 P-glycoprotein inhibitor II Inhibitor 0.5574 Renal organic cation transporter Non-inhibitor 0.7945 CYP450 2C9 substrate Non-substrate 0.8188 CYP450 2D6 substrate Non-substrate 0.8945 CYP450 3A4 substrate Substrate 0.7656 CYP450 1A2 substrate Non-inhibitor 0.8249 CYP450 2C9 inhibitor Non-inhibitor 0.8802 CYP450 2D6 inhibitor Non-inhibitor 0.9434 CYP450 2C19 inhibitor Non-inhibitor 0.7466 CYP450 3A4 inhibitor Non-inhibitor 0.8596 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.5436 Ames test Non AMES toxic 0.9077 Carcinogenicity Non-carcinogens 0.9003 Biodegradation Not ready biodegradable 0.9944 Rat acute toxicity 4.6023 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.7959 hERG inhibition (predictor II) Non-inhibitor 0.8176
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Spectrum Spectrum Type Splash Key Predicted GC-MS Spectrum - GC-MS Predicted GC-MS splash10-0a5l-1019000000-4bbe28a5b3bcf0e3f286 Predicted MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS splash10-0uyi-0139200000-41a77f641ff170d2e2e4 Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS splash10-0002-0009000000-c86dea0eaea17d15e6ed Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS splash10-002b-1109000000-e0db821c3f35e7e3a7c4 Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS splash10-0avi-2139100000-f9520aac8d00101d773c Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS splash10-004i-0409000000-57b8308c805785ff3c7f Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS splash10-074i-3964000000-c8471f03e67b3ac37196 Predicted 1H NMR Spectrum 1D NMR Not Applicable Predicted 13C NMR Spectrum 1D NMR Not Applicable - Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 215.6058044 predictedDarkChem Lite v0.1.0 [M-H]- 202.98143 predictedDeepCCS 1.0 (2019) [M+H]+ 213.4999044 predictedDarkChem Lite v0.1.0 [M+H]+ 204.80632 predictedDeepCCS 1.0 (2019) [M+Na]+ 214.3007044 predictedDarkChem Lite v0.1.0 [M+Na]+ 210.41214 predictedDeepCCS 1.0 (2019)
Targets
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Agonist
- General Function
- Zinc ion binding
- Specific Function
- Nuclear hormone receptor. Transcription factor that mediates the action of vitamin D3 by controlling the expression of hormone sensitive genes. Recruited to promoters via its interaction with BAZ1B...
- Gene Name
- VDR
- Uniprot ID
- P11473
- Uniprot Name
- Vitamin D3 receptor
- Molecular Weight
- 48288.64 Da
References
- Reinhart GA: Vitamin D analogs: novel therapeutic agents for cardiovascular disease? Curr Opin Investig Drugs. 2004 Sep;5(9):947-51. [Article]
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
- Fujishima T, Tsuji G, Tanaka C, Harayama H: Novel vitamin D receptor ligands having a carboxyl group as an anchor to arginine 274 in the ligand-binding domain. J Steroid Biochem Mol Biol. 2010 Jul;121(1-2):60-2. doi: 10.1016/j.jsbmb.2010.04.020. Epub 2010 May 6. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- Iron ion binding
- Specific Function
- Catalyzes the conversion of 25-hydroxyvitamin D3 (25(OH)D) to 1-alpha,25-dihydroxyvitamin D3 (1,25(OH)2D) plays an important role in normal bone growth, calcium metabolism, and tissue differentiation.
- Gene Name
- CYP27B1
- Uniprot ID
- O15528
- Uniprot Name
- 25-hydroxyvitamin D-1 alpha hydroxylase, mitochondrial
- Molecular Weight
- 56503.475 Da
References
- Uchida E, Kagawa N, Sakaki T, Urushino N, Sawada N, Kamakura M, Ohta M, Kato S, Inouye K: Purification and characterization of mouse CYP27B1 overproduced by an Escherichia coli system coexpressing molecular chaperonins GroEL/ES. Biochem Biophys Res Commun. 2004 Oct 15;323(2):505-11. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Curator comments
- Partial agonist.
- General Function
- Zinc ion binding
- Specific Function
- Receptor for retinoic acid. Retinoic acid receptors bind as heterodimers to their target response elements in response to their ligands, all-trans or 9-cis retinoic acid, and regulate gene expressi...
- Gene Name
- RXRA
- Uniprot ID
- P19793
- Uniprot Name
- Retinoic acid receptor RXR-alpha
- Molecular Weight
- 50810.835 Da
References
- Zhang J, Chalmers MJ, Stayrook KR, Burris LL, Garcia-Ordonez RD, Pascal BD, Burris TP, Dodge JA, Griffin PR: Hydrogen/deuterium exchange reveals distinct agonist/partial agonist receptor dynamics within vitamin D receptor/retinoid X receptor heterodimer. Structure. 2010 Oct 13;18(10):1332-41. doi: 10.1016/j.str.2010.07.007. [Article]
Carriers
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Vitamin transporter activity
- Specific Function
- Involved in vitamin D transport and storage, scavenging of extracellular G-actin, enhancement of the chemotactic activity of C5 alpha for neutrophils in inflammation and macrophage activation.
- Gene Name
- GC
- Uniprot ID
- P02774
- Uniprot Name
- Vitamin D-binding protein
- Molecular Weight
- 52963.025 Da
References
- Nykjaer A, Dragun D, Walther D, Vorum H, Jacobsen C, Herz J, Melsen F, Christensen EI, Willnow TE: An endocytic pathway essential for renal uptake and activation of the steroid 25-(OH) vitamin D3. Cell. 1999 Feb 19;96(4):507-15. [Article]
- Verboven C, Rabijns A, De Maeyer M, Van Baelen H, Bouillon R, De Ranter C: A structural basis for the unique binding features of the human vitamin D-binding protein. Nat Struct Biol. 2002 Feb;9(2):131-6. [Article]
- Houghton LA, Vieth R: The case against ergocalciferol (vitamin D2) as a vitamin supplement. Am J Clin Nutr. 2006 Oct;84(4):694-7. [Article]
- Yamamoto N, Naraparaju VR: Vitamin D3-binding protein as a precursor for macrophage activating factor in the inflammation-primed macrophage activation cascade in rats. Cell Immunol. 1996 Jun 15;170(2):161-7. [Article]
- Yamamoto N, Naraparaju VR: Role of vitamin D3-binding protein in activation of mouse macrophages. J Immunol. 1996 Aug 15;157(4):1744-9. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Binder
- General Function
- Not Available
- Specific Function
- Heme binding
- Gene Name
- Not Available
- Uniprot ID
- V9H1D9
- Uniprot Name
- Alpha globin
- Molecular Weight
- 13582.405 Da
References
Drug created at July 26, 2007 12:34 / Updated at February 20, 2024 23:55