cholecalciferol (Vitamin D3)

製品コードS4063 バッチS406304

印刷

化学情報

Synonyms

Cholecalciferol, Colecalciferol

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₂₇H₄₄O

分子量

384.64

CAS No.

67-97-0

Solubility (25°C)*

体外

DMSO

77 mg/mL (200.18 mM)

Ethanol

77 mg/mL (200.18 mM)

Water

Insoluble

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	30%PEG400 1 0.5%Tween80 2 5%propylene glycol この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	30.000mg/ml (78.00mM)	Taking the 1 mL working solution as an example, add 300 μL of 100 mg/ml clarified PEG400 stock solution to 5 μL of Tween80, mix evenly to clarify it; add 50 μL Propylene glycol to the above system, mix evenly to clarify it; then continue to add 645 μL ddH2O to adjust the volume. to 1 mL. The mixed solution should be used immediately for optimal results.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	Cholecalciferol (Vitamin D3, Cholecalciferol, Colecalciferol) is a form of vitamin D, binds and activates a H305F/H397Y mutant vitamin D receptor (VDR) with EC50 of 300 nM.
in vitro	Vitamin D3 is a fat-soluble vitamin that helps your body absorb calcium and phosphorus. Vitamin D3, a precursor in the 1α,25- dihydroxyvitamin D3 biosynthetic pathway, which does not activate wild-type hVDR. It binds and activates H305F/H397Y variant hVDR ,with 70 fold activation in compare to wide-type hVDR. ^[1] Epidemiological studies and work on experimental animals strongly suggest a protective effect of cholecalciferol vitamin D3 (1,25(OH)2D3) against colon cancer and several other cancers. ^[2]
in vivo	With UV-radiation, vitamin D3 is synthesized in the skin from the precursors 7-dehydro-cholesterole and provitamin D3. In the liver, vitamin D3 is transformed to 25-hydroxyvitamin D3. Six cytochrome P450 hydroxylases can exhibit this 25-hydroxylation, with the main enzyme being CYP27A1 (25-hydroxylase). The subsequent step is a 1alpha-hydroxylation by CYP27B1 (1-hydroxylase), which produces the most active form of vitamin D3, 1,25-dihydroxyvitamin-D3. This metabolite is inactivated by a 24-hydroxylation by CYP24 (24-hydro-xylase). Vitamin D3 is used for prevention of mortality in adults. However, Vitamin D3 combines with calcium increased the risk of nephrolithiasis. ^[3]

プロトコル(参考用のみ)

キナーゼアッセイ	Luciferase and β-galactosidase activity assay
キナーゼアッセイ	HEK293T cells are transfected with pCMXwild-type hVDR, pCMXH305F, pCMXH305Y, and pCMXH305F/H397Y. These plasmids contain the Gal4DBD (GBD) fused to the corresponding VDR ligand binding domain (GBD:LBD fusion under the control of a cytomegalovirus (CMV) promoter). The reporter plasmids are p174TATAluc, containing the Renilla* luciferase gene under the control of four Gal4 response elements located upstream from a minimal thymidine kinase promoter, and pCMXβgal, a plasmid containing the β-galactosidase gene under the control of themammalian CMV promoter. The ligands are added to the wells at various concentrations ((0.01 μM– 100 μM) LCA and (0.01 μM–32 μM) cholecalciferol). Cells are harvested and analyzed for luciferase and β-galactosidase activity. Fold activation iscalculated by dividing the value at maximal activation by the value at the no ligand data point.
細胞アッセイ	細胞株	MCF-7
	濃度	~ 100 nM
	反応時間	~ 96 h
	実験の流れ	Vitamin D receptor (VDR)- positive MCF-7 cells in culture are stimulated with the vitamin D metabolites vitamin D3, 25-hydroxyvitamin D3 and 1,25-dihydroxyvitamin D3 for 24, 48, 72 and 96 hours in physiological andsupraphysiological concentrations. The expressions of 25-hydroxylase, 1-hydroxylase and 24-hydroxylase and their changes after stimulation are assessed by real-time PCR.
動物実験	動物モデル	CYP27B1 (−/−) mice
	投薬量	up to 0.625 mg/kg
	投与方法	Oral

参考

https://pubmed.ncbi.nlm.nih.gov/21397016/
http://www.sciencedirect.com/science/article/pii/S0003986110004406
https://pubmed.ncbi.nlm.nih.gov/16886688/

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Vitamin D3 suppresses the cholesterol homeostasis pathway in patient-derived glioma cell lines [ FEBS Open Bio, 2023, 13(9):1789-1806]	PubMed: 37489660
FDA-Approved Drug Screening for Compounds That Facilitate Hematopoietic Stem and Progenitor Cells (HSPCs) Expansion in Zebrafish [ Cells, 2021, 10(8)2149]	PubMed: 34440919
Crosstalk between Hedgehog pathway and the glucocorticoid receptor pathway as a basis for combination therapy in T-cell acute lymphoblastic leukemia [ Oncogene, 2020, 10.1038/s41388-020-01453-2]	PubMed: 32917954

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。