Calcitriol
(Synonyms: 骨化三醇; 1,25-Dihydroxyvitamin D3) 目录号 : GC13852
骨化三醇作为类固醇激素维生素 D 的最具生物活性的代谢产物，抑制骨化三醇会导致抗癌药物的作用降低。
Cas No.:32222-06-3
Sample solution is provided at 25 µL, 10mM.
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 IC?? 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.
| Cell experiment [1]: | |
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Cell lines |
HL-1 cells |
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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. |
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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 experiment [2]: | |
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Animal models |
Male C57BL/6J mice aged 4–5 weeks and weighing ~21–27 g |
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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. |
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Dosage form |
150 IU/kg/day; orally |
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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. |
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References: [1]. Lee TW, et al. Calcitriol downregulates fibroblast growth factor receptor 1 through histone deacetylase activation in HL-1 atrial myocytes. J Biomed Sci. 2018 May 18;25(1):42. [2]. Alkharfy KM, et al. Calcitriol attenuates weight-related systemic inflammation and ultrastructural changes in the liver in a rodent model. Basic Clin Pharmacol Toxicol. 2013 Jan;112(1):42-9. |
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| Cas No. | 32222-06-3 | SDF | |
| 别名 | 骨化三醇; 1,25-Dihydroxyvitamin D3 | ||
| 化学名 | (1R,3S,5Z)-5-[(2E)-2-[(1R,3aS,7aR)-1-[(2R)-6-hydroxy-6-methylheptan-2-yl]-7a-methyl-2,3,3a,5,6,7-hexahydro-1H-inden-4-ylidene]ethylidene]-4-methylidenecyclohexane-1,3-diol | ||
| Canonical SMILES | CC(CCCC(C)(C)O)C1CCC2C1(CCCC2=CC=C3CC(CC(C3=C)O)O)C | ||
| 分子式 | C27H44O3 | 分子量 | 416.64 |
| 溶解度 | ≥ 20.832mg/mL in DMSO | 储存条件 | -20°C, protect from light, stored under nitrogen,unstable in solution, ready to use. |
| General tips | 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；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.4002 mL | 12.0008 mL | 24.0015 mL |
| 5 mM | 0.48 mL | 2.4002 mL | 4.8003 mL |
| 10 mM | 0.24 mL | 1.2001 mL | 2.4002 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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HG + VD group (30 mmol/L D-glucose + 10 nmol/L 1,25(OH)2D3);1,25(OH)2D3 (GLPBIO, Beijing, China) was pretreated for 2 h before intervention.
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Related Biological Data
Effect of vitamin D deficiency on migration of human trophoblast cells. D&E: Cell migration was measured using wound-healing assay. After 12 and 24 h migration, the scratches were photographed and wounded areas were calculated.
And calcitriol (GLPBIO, China) was dissolved in DMSO at the final concentration of 1 mM, and the final concentration of calcitriol were 0.1 μM.
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