| Powder: | Yes |
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| Customized: | Non-Customized |
| Certification: | Enterprise Standards |
| Suitable for: | Adult |
| State: | Powder |
| Purity: | >98% |
| Customization: |
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Active vitamin D drugs are a general term for a series of vitamin D2/D3 derivatives, commonly referred to as "calciferol" drugs. These compounds are complex in structure and involve techniques such as photochemistry and microbial transformation. They are difficult to synthesize, sensitive to light and oxygen, and the API in the preparation is microgram-level, and the development threshold is high. Clinically used mainly for the treatment of osteoporosis, secondary hyperparathyroidism and psoriasis.
Doxercalciferol is a synthetic vitamin D2 analog introduced in the US as Hectorol for the treatment of secondary hyperparathyroidism (SHPT) in patients with end-stage renal failure. It is actually 1-alpha-hydroxyvitamin D2 (one-alpha- D2) and can be synthesized by direct hydroxylation of vitamin D2 tosylate or in 5 steps from ergosterol. Doxercalciferol itself is inactive until metabolized by the liver into active 1,24-dihydroxyvitamin D2, showing a pharmacokinetic profile similar to calcitriol. During placebo-controlled clinical trials, patients with moderate to severe SHPT were treated with 1-alpha-D2 (10 μg doses) for 16 to 24 weeks; in 9 patients out of 10, blood levels of parathyroid hormone were considerably reduced, so maintaining a good control of the parathyroid hyperplasia. Moreover, only a moderate tendency to raise calcium and phosphate was observed. Doxercalciferol is orally-active and less toxic than other vitamin D analogs like alfacalcidol; it shows differentially controlled effects and has an improved safety profile compared to calcitriol.
| Product Name: | Doxercalciferol |
| Synonyms: | 7,10(19),22-tetraene-1,3-diol,(1-alpha,3-beta,5z,7e,22e)-10-secoergosta-5; VITAMIN D2, 1ALPHA-HYDROXY-; Vitamin D2, 1a-Hydroxy-; (1R,3S,5Z)-5-[(2E)-2-[(1R,3aS,7aR)-1-[(E,2R,5R)-5,6-Dimethylhept-3-en-2-yl]-7a-methyl-2,3,3a,5,6,7-hexahydro-1H-inden-4-ylidene]ethylidene]-4-methylidenecyclohexane-1,3-diol; A, 25-DIHYDROXYERGOCALCIFEROL; 1A-HYDROXYERGOCALCIFEROL (NON GMP); ERCALCIDOL |
| CAS: | 54573-75-0 |
| MF: | C28H44O2 |
| MW: | 412.65 |
| Product Categories: | Vitamin D3 analogs;Chiral Reagents;Inhibitors;-;Intermediates & Fine Chemicals;Pharmaceuticals |
| Quality Standard: | USP41*Y20180001141 |
| Molecular Structure: | |
| Melting point | 138-140°C |
| Storage temp. | Desiccate at -20°C |
| Solubility | DMSO: >10mg/mL |
| Form | White crystalline powder |
Uses
Synthetic vitamin D prohormone. A new active Vitamin D analog which inhibits growth of human neuroblastoma.
Doxercalciferol is a synthetic vitamin D2 analog, suppressing parathyroid synthesis and secretion, used to treat secondary hyperparathyroidism and metabolic bone disease.
1)Doxercalciferol (100 or 300 pg/g b.w.) normalizes serum calcium and parathyroid hormone (PTH) levels in nephrectomy treated mice. Doxercalciferol (300 pg/g b.w.) significantly reduces osteitis fibrosa in nephrectomy treated mice.
2)Doxercalciferol results in significant decrease in cardiac hypertrophy and improves cardiac function in rats fed a high salt (HS) diet. Doxercalciferol treatment leads to a significant decrease in plasma brain natriuretic peptide (BNP) level and tissue atrial natriuretic factor (ANF) mRNA level in rats fed a high salt (HS) diet. Doxercalciferol also significantly reduces the level of protein kinase C-α (PKCα) suggesting that PKC-mediated cardiac hypertrophy may be associated with vitamin D deficiency.
3)Doxercalciferol decreases proteinuria, podocyte injury, mesangial expansion, and extracellular matrix protein accumulation in Diet-induced obesity (DIO) mice. Doxercalciferol also decreases macrophage infiltration, oxidative stress, proinflammatory cytokines, and profibrotic growth factors in DIO mice. Doxercalciferol also prevents the activation of the renin-angiotensin-aldosterone system including the angiotensin II type 1 receptor and the mineralocorticoid receptor in DIO mice.
4)Doxercalciferol combined with Losartan most effectively prevents albuminuria, restored glomerular filtration barrier structure, and dramatically reduces glomerulosclerosis in a dose-dependent manner in mice. Doxercalciferol combined with Losartan virtually prevents morphological and molecular changes in diabetic kidneys of mice.
Only for Research & Lab Use,not for human use.
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