骨化三醇作用機制 - Medchemexpress - MCE中國

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

2、gen)溶解性數(shù)據(jù)體外實驗 DMSO : 100 mg/mL (240.02 mM)* means soluble, but saturation unknown.SolventMass1 mg 5 mg 10 mgConcentration制備儲備液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請根據(jù)產品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；旦配成溶液，請分裝保存，避免反復凍融造成的產品失效。儲備液的保存式和期限：-80C

3、, 6 months; -20C, 1 month (protect from light, stored under nitrogen)。-80C 儲存時，請在 6 個內使，-20C 儲存時，請在 1 個內使。體內實驗請根據(jù)您的實驗動物和給藥式選擇適當?shù)娜芙獍浮Ｒ韵氯芙獍付颊埾劝凑?In Vitro 式配制澄清的儲備液，再依次添加助溶劑：為保證實驗結果的可靠性，澄 的儲備液可以根據(jù)儲存條件，適當保存；體內實驗的作液，建議您現(xiàn)現(xiàn)配，當天使； 以下溶劑前顯的百分 指該溶劑在您配制終溶液中的體積占；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的式助溶1. 請依序添加每種溶劑： 10%

4、DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (6.00 mM); Clear solution此案可獲得 2.5 mg/mL (6.00 mM，飽和度未知) 的澄清溶液。以 1 mL 作液為例，取 100 L 25.0 mg/mL 的澄 DMSO 儲備液加到 400 L PEG300 中，混合均勻；向上述體系中加50 L Tween-80，混合均勻；然后繼續(xù)加 450 L 理鹽定容 1 mL。2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5

5、 mg/mL (6.00 mM); Clear solution此案可獲得 2.5 mg/mL (6.00 mM，飽和度未知) 的澄清溶液。Page 1 of 2 www.MedChemE以 1 mL 作液為例，取 100 L 25.0 mg/mL 的澄均勻。DMSO 儲備液加到 900 L 20% 的 SBE-CD 理鹽溶液中，混合3. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (6.00 mM); Clear solution此案可獲得 2.5 mg/mL (6.00 mM，飽和度未知) 的澄 溶液，此案不適于實驗周 期在半

6、個以上的實驗。以 1 mL 作液為例，取 100 L 25.0 mg/mL 的澄 DMSO 儲備液加到 900 L 油中，混合均勻。BIOLOGICAL ACTIVITY物活性 Calcitriol活性最的 vitamin D 代謝物，也是vitamin D 受體 (VDR) 的激動劑。IC & Target Human Endogenous Metabolite體外研究 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.體內研究 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戶使本產品發(fā)表的科研獻 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