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| Cas No.: | 54573-75-0 |
| Chemical Name: | Vitamin D2, 1a-Hydroxy- |
| Synonyms: | Vitamin D2, 1a-Hydroxy-;1α-hydroxyergocalciferol (Ercalcidol);1ALPHA-OH-D2;1-alpha-hydroxyergocalciferol;1alpha-hydroxyergocalciferol;1-alpha-hydroxyvitamind2;1-hydroxyergocalciferol;7,10(19),22-tetraene-1,3-diol,(1-alpha,3-beta,5z,7e,22e)-10-secoergosta-5;VITAMIN D2, 1ALPHA-HYDROXY-;25-HYDROXYERGOCALCIFEROL;Doxercalciferol;(1R,3S,E)-5-((E)-2-((1R,3AS,7aR)-1-((2R,5S,E)-5,6-dimethylhept-3-en-2-yl)-7a-methyldihydro-1H-inden-4(2H,5H,6H,7H,7aH)-ylidene)ethylidene)-4-methylenecyclohexa;1.alpha.-Hydroxyvitamin D2;1-hydroxy Vitamin D2;Doxecalciferol;(5Z,7E,22E)-9,10-Secoergosta-5,7,10(19),22-tetraene-1α,3β-diol;(5Z,7E,22E)-9,10-Secoergosta-5,7,10(19),22-tetraene-1,3-diol;1α-Hydroxyergocalciferol;1α-Hydroxyvitamin D2;1α-OHD2;1-α-Hydroxyvitamin D2;1-Hydroxyergocalciferol;TSA 840;(5Z,7E,22E)-9,10-Secoergosta-5,7,10,22-tetraene-1,3-diol;(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;1α-Hydroxy Vitamin D2 |
| SMILES: | CC([C@H](/C=C/[C@H]([C@H]1CC[C@H]2/C(=C/C=C3/C[C@@H](O)C[C@H](O)C/3=C)/CCC[C@]12C)C)C)C |
| Formula: | C28H44O2 |
| M.Wt: | 412.647768974304 |
| Purity: | >99% |
| Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
| Description: | Doxercalciferol is a Vitamin D2 analog, acts as an activator of Vitamin D receptor, and prevent renal disease. |
| Target: | Vitamin D receptor[1] |
| In Vivo: | Doxercalciferol (0.083, 0.167 or 0.333 μg/kg, i.p.) elevates serum phosphorus at Week 6 in 5/6 nephrectomized (NX) rats. Doxercalciferol (0.167 and 0.333 μg/kg) also increases serum calcium and Ca × P at Weeks 2 and 6, and enhances increased pulse wave velocity (PWV) at Week 6 in 5/6 nephrectomized (NX) rats. Doxercalciferol blocks PTH from rising at 0.083 μg/kg, and lowers serum PTH to the SHAM level[1]. Doxercalciferol (125 ng/kg, i.p. thrice per week) increases expression of VDR mRNA level and renal expression of TRPV5 in NON mice fed a HF diet. Doxercalciferol also improves proteinuria, prevents loss of podocytes, and accumulation of extracellular matrix proteins in HF diet-induced mice. Doxercalciferol inhibits the expression of profibrotic growth factors (TGF-β, PAI-1, and connective tissue growth factor (CTGF)), and blocks increased expression of the renin-angiotensin-aldosterone system in mice fed a HF diet. Furthermore, Doxercalciferol suppresses macrophage infiltration, decreases NF-κb activity, and preventes expression of proinflammatory cytokine and the increase in renal lipid accumulation in mice fed a HF diet[2]. Doxercalciferol (30 ng/kg, i.p. thrice per week) prevents albuminuria, markedly attenuates podocyte loss and apoptosis, and reduces glomerular fibrosis in streptozotocin-induced diabetic mice[3]. |
| Animal Administration: | Rats[1] Male, Sprague-Dawley, 5/6 nephrectomized (NX) rats (∼200 gm) are used 1 week after nephrectomy. The nephrectomy is performed using a standard two-step surgical ablation procedure. Beginning 2 weeks post-nephrectomy, rats are maintained on a high phosphorus diet (0.9% phosphorus and 0.6% calcium) for the duration of the study to induce secondary hyperparathyroidism. On Day 0, SHAM and 5/6 NX rats (n = 7-10 per group) receive vehicle (5% EtOH/95% propylene glycol; 0.4 mL/kg; i.p.) or VDRA (paricalcitol or Doxercalciferol; 0.083, 0.167 or 0.333 μg/kg; intraperitoneally) three times per week for 41 days (n = 6-10 per group). These doses are chosen based on the fact that lower doses (0.021 and 0.042 μg/kg; i.p.) of either compound are not PTH suppressive after 2 or 6 weeks of treatment in this model of CKD. On Days 0, 13 and 41, blood is collected (24 h post-dose). On Days 0, 13 and 41 (24 h post-dose), animals are anaesthetized with ketamine (50 mg/kg) and blood is collected via the tail vein for PTH and serum blood chemistry determinations[1]. |
| References: | [1]. Noonan W, et al. Differential effects of vitamin D receptor activators on aortic calcification and pulse wave velocity in uraemic rats. Nephrol Dial Transplant. 2008 Dec;23(12):3824-30. [2]. Wang XX, et al. Vitamin D receptor agonist doxercalciferol modulates dietary fat-induced renal disease and renal lipid metabolism. Am J Physiol Renal Physiol. 2011 Mar;300(3):F801-10. [3]. Wang Y, et al. Vitamin D receptor signaling in podocytes protects against diabetic nephropathy. J Am Soc Nephrol. 2012 Dec;23(12):1977-86. |
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COA
| LOT NO. | DOWNLOAD |
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| 2018-0101 |
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| 2018-0101 |
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| 2018-0101 |
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