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Calcitriol
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Calcitriol图片
包装与价格:
包装价格(元)
2mg电议
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
骨化三醇是维生素 D 最活跃的代谢物,也是维生素 D 受体 (VDR) 激动剂。

Cell lines

HL-1 cells

Preparation Method

Calcitriol (1 and 10 nM) was used to treat HL-1 cells for 48 h to determine the initial dose-response effect. To study the functional relevance of FGFR1 modulation, recombinant mouse FGF-2 (25 ng/mL) was administrated (for 0.5 or 48 h) in control and calcitriol-treated HL-1 cells.

Reaction Conditions

1 and 10 nM; 48 h

Applications

Compared to control cells, as shown in Fig. 1a, calcitriol (1 and 10 nM) dose-dependently reduced FGFR1 protein expression in HL-1 cells by 31 and 62%, respectively. Similarly, calcitriol (10 nM)-treated HL-1 cells had lower FGFR1 mRNA expression than did control HL-1 cells.

Animal models

Male C57BL/6J mice aged 4–5 weeks and weighing ~21–27 g

Preparation Method

Four groups of mice (n = 11 each) were maintained on either low-fat diet (LFD) or high-fat diet (HFD) with and without 150 IU/kg/day calcitriol orally for 16 weeks.

Dosage form

150 IU/kg/day; orally

Applications

A significant gradual decrease in weight was observed in HFD-fed mice treated with calcitriol compared with a steady increase in controls. Furthermore, calcitriol treatment reduced concentrations of various inflammatory markers including TNF-α, CRP and IL-6.

文献引用
产品描述

Calcitriol, as the most biologically active metabolite derived from the secosteroid hormone vitamin D, the inhibition of calcitriol caused decreased effects of anticancer drugs.[1]

In vitro efficacy test it shown that weekly oral administration of calcitriol allowed reach the peak serum calcitriol concentrations well above 1 nM, a concentration that inhibition more than 50% of prostate cancer proliferation.[2]With 10 nM calcitriol remarkably decreased RAGE protein expression and increased sRAGE concentrations in HL-1 cardiomyocytes compared with control cells.[3]Calcitriol exhibited antiproliferative effects against T47D, MCF-7, and MDA-MB-231 with IC50 values in the range of 0.05-0.25 μM.[4] In addition, calcitriol inhibits melanoma cell proliferation with an IC50 of 0.24 μM.[5]BT-474 cells were dose-dependently growth-inhibited by calcitriol with IC50 of 2.9 nM. With 1 nM Calcitriol synergistically improved AZD4547 antiproliferative effects, allowing a 2-fold AZD4547 dose-reduction.[6]

In vivo test it demonstrated that calcitriol (0.03 μg/kg) 5 times/wk intraperitoneally for 10 wk in UNX ApoE-/- mice caused significant vascular calcification and elevated expression of related proteins (BMP2, RANKL, and Runx2).[8]With 0.5 ug/day calcitriol orally improved insulin resistance and HOMA-β after 6 months in ND patients, however, only improved HOMA-β in the dialysis patients, with no obvious effect on insulin resistance.[7]

References:
[1]Ma J, et al. The mechanism of calcitriol in cancer prevention and treatment. Curr Med Chem. 2013;20(33):4121-30.
[2]Beer TM. Development of weekly high-dose calcitriol based therapy for prostate cancer. Urol Oncol. 2003 Sep-Oct;21(5):399-405.
[3]Lee TW, et al. ADAM10 modulates calcitriol-regulated RAGE in cardiomyocytes. Eur J Clin Invest. 2017 Sep;47(9):675-683.
[4]Aljunidee KA, et al. Combination therapy of calcitriol inhibits the proliferation of breast cancer cells: new concept of nonclassical function of calcitriol. Horm Mol Biol Clin Investig. 2021 Nov 15.
[5]Sutedja EK, et al. Calcitriol Inhibits Proliferation and Potentially Induces Apoptosis in B16-F10 Cells. Med Sci Monit Basic Res. 2022 May 5;28:e935139.
[6]Morales-Guadarrama G, et al. AZD4547 and calcitriol synergistically inhibited BT-474 cell proliferation while modified stemness and tumorsphere formation. J Steroid Biochem Mol Biol. 2022 May 31;223:106132.
[7]Lu Y, et al. Effects of active vitamin D on insulin resistance and islet β-cell function in non-diabetic chronic kidney disease patients: a randomized controlled study. Int Urol Nephrol. 2022 Jul;54(7):1725-1732.
[8]Becker LE, et al. Effect of paricalcitol and calcitriol on aortic wall remodeling in uninephrectomized ApoE knockout mice. Am J Physiol Renal Physiol. 2011 Mar;300(3):F772-82.