Calcifediol
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
维生素D受体(VDR)活化对慢性肾病病人的心血管和生存有益.Calcifediol也称calcidiol,是一种在肝脏中对维生素D3进行羟基化而产生的前激素.
在体外:Calcifediol可诱导CYP24A1表达,EC50值为70 nM.Calcifediol可刺激血栓调节蛋白表达,EC50值为10-100 nM.共聚焦显微镜表明0.1 - 10 μM的calcifediol可剂量依赖地诱导VDR转移到细胞核中;这种VDR转移模式与calcitriol处理的细胞中的情形相似[1].
在体内:给自发性高血压大鼠和血压正常的Wistar-Kyoto(WKY)大鼠注射50 ng/d的calcifediol或单纯溶剂3天.对照SHR出现了钙结合蛋白-D9K和细胞Ca2+流下降.Calcifediol可提高总细胞量和刷状缘钙结合蛋白-D9K.相比,在vit-D动物中提高的Ca2+流在SHR中维持低水平,血浆骨化三醇水平与WKY大鼠中的相似[2].
临床试验:Calcifediol每日\每周或单次推注给药提高血浆25(OH)D3浓度,比维生素D3有效2-3倍.对calcifediol而言,达到30 ng/mL的血浆25(OH)D3浓度更为快速可靠[3].
参考文献:
[1] Wu-Wong JR, Chen YW, Nakane M, Wolf M. Differential effects of vitamin d receptor agonists on gene expression in neonatal rat cardiomyocytes. Cardiovasc Drugs Ther. 2011 Jun;25(3):215-22.
[2] Roullet CM, Roullet JB, Martin AS, McCarron DA. In vivo effect of calcitriol on calcium transport and calcium binding proteins in the spontaneously hypertensive rat. Hypertension. 1994 Aug;24(2):176-82.
[3] Jetter A, Egli A, Dawson-Hughes B, Staehelin HB, Stoecklin E, Goessl R, Henschkowski J, Bischoff-Ferrari HA. Pharmacokinetics of oral vitamin D(3) and calcifediol. Bone. 2014 Feb;59:14-9.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 400.64 |
Cas No. | 19356-17-3 |
Formula | C27H44O2 |
Solubility | insoluble in H2O; ≥13.65 mg/mL in DMSO; ≥41.2 mg/mL in EtOH |
Chemical Name | (1S,3Z)-3-[(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-methylidenecyclohexan-1-ol |
SDF | Download SDF |
Canonical SMILES | CC(CCCC(C)(C)O)C1CCC2C1(CCCC2=CC=C3CC(CCC3=C)O)C |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
细胞实验 [1,2]: | |
细胞系 |
新生大鼠心肌细胞,浆细胞样树突状细胞(pDC)和常规DCs |
溶解方法 |
该化合物在DMSO中的溶解度大于13.65 mg/mL。若获取更高浓度的溶液,可在37℃下孵育10分钟,随后在超声波浴中摇匀。-20℃以下可储存数月。 |
反应条件 |
0.1-10 μM,2小时 |
应用 |
Calcifediol诱导CYP24A1表达,EC50为70 nM。Calcifediol刺激血栓调节蛋白的表达。EC50为10-100 nM。Calcifediol(0.1-10 μM)以剂量依赖性方式诱导VDR移位入细胞核。在moDC中,Calcifediol治疗16小时后显著诱导Cyp24A1表达。 |
动物实验 [2]: | |
动物模型 |
Wistar-Kyoto大鼠 |
给药剂量 |
50 ng/d,3天 |
应用 |
在自发性高血压大鼠和血压正常的Wistar-Kyoto(WKY)大鼠中,50 ng/d剂量的calcifediol给药3天,增加总细胞和钙结合蛋白D9K水平。 |
注意事项 |
由于实验环境的不同,实际溶解度可能与理论值略有不同,请测试室内所有化合物的溶解度。 |
References: [1]. Wu-Wong J R, Chen Y W, Nakane M, et al. Differential effects of vitamin d receptor agonists on gene expression in neonatal rat cardiomyocytes[J]. Cardiovascular drugs and therapy, 2011, 25(3): 215-222. [2]. Karthaus N, Van Spriel A B, Looman M W G, et al. Vitamin D controls murine and human plasmacytoid dendritic cell function[J]. Journal of Investigative Dermatology, 2014, 134(5): 1255-1264. [3]. Roullet C M, Roullet J B, Martin A S, et al. In vivo effect of calcitriol on calcium transport and calcium binding proteins in the spontaneously hypertensive rat[J]. Hypertension, 1994, 24(2): 176-182. |
质量控制和MSDS
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