骨化三醇作用机制 - Medchemexpress - MCE中国

1、Product Data SheetCalcitriolCat. No.: HY-10002CAS No.: 32222-06-3分式: CHO分量: 416.64作靶点: VD/VDR; Endogenous Metabolite作通路: Vitamin D Related; Metabolic Enzyme/Protease储存式: -20C, protect from light, stored under nitrogen* In solvent : -80C, 6 months; -20C, 1 month (protect from light, stored undernitro

2、gen)溶解性数据体外实验 DMSO : 100 mg/mL (240.02 mM)* means soluble, but saturation unknown.SolventMass1 mg 5 mg 10 mgConcentration制备储备液1 mM 2.4002 mL 12.0008 mL 24.0015 mL5 mM 0.4800 mL 2.4002 mL 4.8003 mL10 mM 0.2400 mL 1.2001 mL 2.4002 mL请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存式和期限：-80C

3、, 6 months; -20C, 1 month (protect from light, stored under nitrogen)。-80C 储存时，请在 6 个内使，-20C 储存时，请在 1 个内使。体内实验请根据您的实验动物和给药式选择适当的溶解案。以下溶解案都请先按照 In Vitro 式配制澄清的储备液，再依次添加助溶剂：为保证实验结果的可靠性，澄 的储备液可以根据储存条件，适当保存；体内实验的作液，建议您现现配，当天使； 以下溶剂前显的百分 指该溶剂在您配制终溶液中的体积占；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的式助溶1. 请依序添加每种溶剂： 10%

4、DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (6.00 mM); Clear solution此案可获得 2.5 mg/mL (6.00 mM，饱和度未知) 的澄清溶液。以 1 mL 作液为例，取 100 L 25.0 mg/mL 的澄 DMSO 储备液加到 400 L PEG300 中，混合均匀；向上述体系中加50 L Tween-80，混合均匀；然后继续加 450 L 理盐定容 1 mL。2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5

5、 mg/mL (6.00 mM); Clear solution此案可获得 2.5 mg/mL (6.00 mM，饱和度未知) 的澄清溶液。Page 1 of 2 www.MedChemE以 1 mL 作液为例，取 100 L 25.0 mg/mL 的澄均匀。DMSO 储备液加到 900 L 20% 的 SBE-CD 理盐溶液中，混合3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (6.00 mM); Clear solution此案可获得 2.5 mg/mL (6.00 mM，饱和度未知) 的澄 溶液，此案不适于实验周 期在半

6、个以上的实验。以 1 mL 作液为例，取 100 L 25.0 mg/mL 的澄 DMSO 储备液加到 900 L 油中，混合均匀。BIOLOGICAL ACTIVITY物活性 Calcitriol活性最的 vitamin D 代谢物，也是vitamin D 受体 (VDR) 的激动剂。IC & Target Human Endogenous Metabolite体外研究 Calcitriol exerts antiproliferative effects on cervical cancer cells in vitro. Cells decrease by 12.8% when trea

7、ted with 100nM Calcitriol for 6 days, compare with control. Inhibition of cell proliferation becomes more pronounced with theincrease in Calcitriol concentration. The decrease is 26.1% and 31.6% for 200 and 500 nM Calcitriol, respectively.Treatment with Calcitriol for 72 h induces an evident accumul

8、ation of cells in the G1 phase, with approximately66.18% in 200 nM and 78.10% in 500 nM, compare with the control (24.36%). Calcitriol treatment significantlydecreases HCCR-1 protein expression compare with the control in a time- and dose-dependent manner1. Calcitriolsignificantly increases ER mRNA

9、in a dose dependent manner with an EC50 of 9.810-9 M2.体内研究 Chronic treatment with Calcitriol (150 ng/kg per day for 4.5 months) improves the relaxations (pD2: 6.300.09, Emax:68.63.9% in Calcitriol-treated OVX, n=8). Renal blood flow in OVX rats is reduced in both kidneys, and the flow isrestored by

10、Calcitriol treatment. The increased expression of COX-2 and Thromboxane-prostanoid (TP) receptor inOVX rat renal arteries is reduced by chronic calcitriol administration3. High- and low-dose Calcitriol treatmentsignificantly decreases the systolic blood pressure (SBP) in the fructose-fed rats by 144

11、 and 94 mmHg, respectively,at Day 56. High-dose Calcitriol treatment (20 ng/kg per day) significantly increases serum ionized calcium level(1.440.05 mmol/L) compare with the other groups4.PROTOCOLCell Assay 1 HeLa S3 cells are plated at a density of 1,000 cells/well in 96-well plates of Dulbeccos mo

12、dified Eagles medium(DMEM) with 10% fetal bovine serum (FBS), treated with 1% ethanol (control) or various concentrations of Calcitriol (100, 200, and 500 nM) for 72 h. A Cell Counting Kit8 (CCK-8) is used to determine cell proliferation. At 24, 48, 72, 96,120, and 144 h after culturing with 200 nM

13、Calcitriol, cells are harvested for analysis. Three independent experimentsare performed in quadruplicate1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Adult female Sprague-Dawley rats weighing 200 to 220g are used in this study. Rats are hous

14、ed in a temperature-Administration 3 controlled room (23C) with a 12-h light/dark cycle. The animals have free access to a standard diet and water.Ovariectomy (OVX) is performed on rats. At 6 months after the surgical procedure, the OVX rats are randomlyassigned to either treatment with vehicle dime

15、thyl sulfoxide (OVX+vehicle) or Calcitriol (150 ng/kg daily,OVX+calcitriol). Calcitriol treatment is given by oral gavage and lasted or 4.5 months. Blood pressure and serumCalcitriol level are measured3.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Pa

16、ge 2 of 3 www.MedChemE户使本产品发表的科研献 J Lipid Res. 2019 Mar 22. pii: jlr.D092197. J Steroid Biochem Mol Biol. 2017 Oct;173:341-348. Cell Signal. 2020 Feb 6:109567. Int Immunopharmacol. 2017 Apr 13;47:182-189. Biomed Chromatogr. 2020 Jan 3:e4783.See more customer validations on HYPERLINK www.MedChemE www

17、.MedChemEREFERENCES1. Wang G, et al. Calcitriol Inhibits Cervical Cancer Cell Proliferation Through Downregulation of HCCR1 Expression. Oncol Res. 2014;22(5-6):301-9.2. Santos-Martnez N, et al. Calcitriol restores antiestrogen responsiveness in estrogen receptor negative breast cancer cells: a poten

18、tial new therapeuticapproach. BMC Cancer. 2014 Mar 29;14:230.3. Dong J, et al. Calcitriol restores renovascular function in estrogen-deficient rats through downregulation of cyclooxygenase-2 and the thromboxane-prostanoid receptor. Kidney Int. 2013 Jul;84(1):54-63.4. Chou CL, et al. Beneficial effects of calcitriol on hypertension, glucose intolerance, impairment of endothelium-dependent vascular relaxation, andvisceral adiposity in fructose-fe