|Related Categories||Cell Biology, Cell Signaling and Neuroscience, Gene Regulation, Gene Regulation and Expression, Metabolic Pathways,|
|solubility||DMSO: >10 mg/mL|
|shipped in||wet ice|
Doxercalciferol is a Vitamin D2 analogue, a Vitamin D Receptor Activator (VDRA). Doxercalciferol acts as a pro-hormone, needing 25-hydroxylation in the liver for bioactivation into 1α, 25-hydroxyvitamin D2. Pivotal studies in adults on dialysis have demonstrated control of secondary hyperparathyroidism that is superior to placebo therapy, without undue suppression of 1st IMA-PTH < 300 pg/mL, or occurrences of hypercalcemia. Doxercalciferol has been shown to be effective in controlling secondary hyperparathyroidism of adult patients with CKD stages 3-4.
Doxercalciferol is a vitamin D2 analog that acts as a pro-hormone, activated in the liver to 1α,25-dihydroxyvitamin D2. Despite its relatively low affinity for the vitamin D receptor (VDR) (before activation), it is effective at suppressing expression of the parathyroid hormone (PTH) gene, and appears to act through the VDR.
Phase II open label, multi-center clinical trial of modulation of intermediate endpoint biomarkers by 1α-hydroxyvitamin D2 in patients with clinically localized prostate cancer and high grade pin. Gee J, Bailey H, Kim K, et al. Prostate 73(9), 970-8, (2013)
Vitamin D receptor agonist doxercalciferol modulates dietary fat-induced renal disease and renal lipid metabolism. Wang XX, Jiang T, Shen Y, et al. Am. J. Physiol. Renal Physiol. 300(3), F801-10, (2011)
Kidney bone disease and mortality in CKD: revisiting the role of vitamin D, calcimimetics, alkaline phosphatase, and minerals. Kalantar-Zadeh K, Shah A, Duong U, et al. Kidney Int. Suppl. (117), S10-21, (2010)
Converting hemodialysis patients from intravenous paricalcitol to intravenous doxercalciferol - a dose equivalency and titration study. Fadem SZ, Al-Saghir F, Zollner G, et al. Clin. Nephrol. 70(4), 319-24, (2008)
Real-world doxercalciferol treatment in SHPT CKD stage 3 and 4: an analysis of change in iPTH and accordance to KDOQI recommendations. Kumar N, Lindberg J, David K, et al. Am. J. Nephrol. 29(2), 71-8, (2009)
Differential effects of vitamin D receptor activators on aortic calcification and pulse wave velocity in uraemic rats. Noonan W, Koch K, Nakane M, et al. Nephrol. Dial. Transplant. 23(12), 3824-30, (2008)
Calcitriol and doxercalciferol are equivalent in controlling bone turnover, suppressing parathyroid hormone, and increasing fibroblast growth factor-23 in secondary hyperparathyroidism. Wesseling-Perry K, Pereira RC, Sahney S, et al. Kidney Int. 79(1), 112-9, (2011)
Calcium balance in dialysis is best managed by adjusting dialysate calcium guided by kinetic modeling of the interrelationship between calcium intake, dose of vitamin D analogues and the dialysate calcium concentration. Gotch F, Levin NW, and Kotanko P Blood Purif. 29(2), 163-76, (2010)
A randomized trial of cholecalciferol versus doxercalciferol for lowering parathyroid hormone in chronic kidney disease. Moe SM, Saifullah A, LaClair RE, et al. Clin. J. Am. Soc. Nephrol. 5(2), 299-306, (2010)
Long-term therapeutic effect of vitamin D analog doxercalciferol on diabetic nephropathy: strong synergism with AT1 receptor antagonist. Zhang Y, Deb DK, Kong J, et al. Am. J. Physiol. Renal Physiol. 297(3), F791-801, (2009)
Randomized, double-blinded phase II evaluation of docetaxel with or without doxercalciferol in patients with metastatic, androgen-independent prostate cancer. Attia S, Eickhoff J, Wilding G, et al. Clin. Cancer Res. 14(8), 2437-43, (2008)
Direct suppression of Pth gene expression by the vitamin D prohormones doxercalciferol and calcidiol requires the vitamin D receptor Ritter, C.S., and Brown, A.J. J. Mol. Endocrinol. 46, 63-66, (2011)
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