骨化三醇的杂质 B,骨化三醇 (1,25-二羟基维生素 D3;Rocaltrol) 是维生素 D 的激素活性形式,骨化三醇是维生素 D3 的活性代谢物,可激活维生素 D 受体 (VDR)。
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Impurity B of Calcitriol, Calcitriol(1,25-Dihydroxyvitamin D3; Rocaltrol ) is the hormonally active form of vitamin D, Calcitriol is the active metabolite of vitamin D3 that activates the vitamin D receptor (VDR).IC50 value:Target: vitamin D receptorCalcitriol(1,25-Dihydroxyvitamin D3; Rocaltrol ) displays calcemic actions. Calcitriol stimulates intestinal and renal Ca2+ absorption and regulates bone Ca2+ turnover. Calcitriol (1,25-Dihydroxyvitamin D3; Rocaltrol )exhibits antitumor activity; Calcitriol(1,25-Dihydroxyvitamin D3; Rocaltrol ) inhibits in vivo and in vitro cell proliferation in a wide range of cells including breast, prostate, colon, skin and brain carcinomas and myeloid leukemia cells.
参考文献:
[1]. Canalejo et al (2000) The in vitro effect of calcitriol on parathyroid cell proliferation and apoptosis. J.Am.Soc.Nephrol. 11 1865. Beer and Myrthue (2004)
[2]. Calcitriol in cancer treatment: from the lab to the clinic. Mol.Cancer Ther. 3 373.
[3]. Krishnan AV, Swami S, Feldman D.Equivalent anticancer activities of dietary vitamin D and calcitriol in an animal model of breast cancer: Importance of mammary CYP27B1 for treatment and prevention.J Steroid Biochem Mol Biol. 2012 Aug 23.
[4]. Alkharfy KM, Al-Daghri NM, Yakout SM, Ahmed M. Calcitriol Attenuates Weight-Related Systemic Inflammation and Ultrastructural Changes of the Liver in a Rodent Model.Basic Clin Pharmacol Toxicol. 2012 Aug 21.
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