Calcitriol

製品コードS1466 バッチS146603

化学情報

	Synonyms	RO215535, Topitriol, 1,25-Dihydroxyvitamin D3	Storage (From the date of receipt)	1 year -80°C powder（in dark and seal）
	化学式	C₂₇H₄₄O₃
	分子量	416.64	CAS No.	32222-06-3
Solubility (25°C)*	体外	DMSO	83 mg/mL (199.21 mM)
		Ethanol	83 mg/mL (199.21 mM)
		Water	Insoluble
* <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	Calcitriol is a nonselective vitamin D receptor activator/agonist(VDRA), exhibiting a 10-fold higher vitamin D receptor (VDR) binding affinity(IC50=0.4 nM) than the selective VDRA paricalcitol.Solutions are unstable and should be fresh-prepared.
in vitro	Calcitriol is a potent inhibitor of PHA-induced lymphocyte proliferation, achieving 70% inhibition of tritiated thymidine incorporation after 72 h in culture. Calcitriol suppresses interleukin-2 (IL-2) production by PHA-stimulated peripheral blood mononuclear cells in a concentration-dependent fashion. ^[1] Calcitriol increases the concentration of intracellular calcium ([Ca2+]i) within 5 s by mobilizing calcium from the endoplasmic reticulum and the formation of inositol 1,4, 5-trisphosphate and diacylglycerol. ^[2] Calcitriol can inhibit the proliferation and promote the differentiation of human prostate adenocarcinoma cells. Calcitriol causes a selective decrease in the secreted levels of type IV collagenases (MMP-2 and MMP-9). ^[3] Calcitriol has antiproliferative activity in squamous cell carcinoma and prostatic adenocarcinoma and enhances the antitumor activity of platinum-based agents. Calcitriol prior to paclitaxel significantly reduces clonogenic survival compared with either agent alone in the murine squamous cell carcinoma and PC-3 cells. ^[4] Calcitriol is a potent anti-proliferative agent in a wide variety of malignant cell types. Calcitriol effects are associated with an increase in G0/G1 arrest, induction of apoptosis and differentiation, modulation of expression of growth factor receptors. Calcitriol potentiates the antitumor effects of many cytotoxic agents and inhibits motility and invasiveness of tumor cells and formation of new blood vessels. ^[5]

製品説明

Calcitriol is a nonselective vitamin D receptor activator/agonist(VDRA), exhibiting a 10-fold higher vitamin D receptor (VDR) binding affinity(IC50=0.4 nM) than the selective VDRA paricalcitol.Solutions are unstable and should be fresh-prepared.

in vitro

Calcitriol is a potent inhibitor of PHA-induced lymphocyte proliferation, achieving 70% inhibition of tritiated thymidine incorporation after 72 h in culture. Calcitriol suppresses interleukin-2 (IL-2) production by PHA-stimulated peripheral blood mononuclear cells in a concentration-dependent fashion. ^[1]

Calcitriol increases the concentration of intracellular calcium ([Ca2+]i) within 5 s by mobilizing calcium from the endoplasmic reticulum and the formation of inositol 1,4, 5-trisphosphate and diacylglycerol. ^[2]

Calcitriol can inhibit the proliferation and promote the differentiation of human prostate adenocarcinoma cells. Calcitriol causes a selective decrease in the secreted levels of type IV collagenases (MMP-2 and MMP-9). ^[3]

Calcitriol has antiproliferative activity in squamous cell carcinoma and prostatic adenocarcinoma and enhances the antitumor activity of platinum-based agents. Calcitriol prior to paclitaxel significantly reduces clonogenic survival compared with either agent alone in the murine squamous cell carcinoma and PC-3 cells. ^[4]

Calcitriol is a potent anti-proliferative agent in a wide variety of malignant cell types. Calcitriol effects are associated with an increase in G0/G1 arrest, induction of apoptosis and differentiation, modulation of expression of growth factor receptors. Calcitriol potentiates the antitumor effects of many cytotoxic agents and inhibits motility and invasiveness of tumor cells and formation of new blood vessels. ^[5]

プロトコル(参考用のみ)

細胞アッセイ	細胞株	CLL cells
	濃度	100 nM
	反応時間	24 h
	実験の流れ	CLL cells were treated with DMSO (vehicle control) or calcitriol (100 nM). Cells were harvested at the indicated time points with mild trypsinization
動物実験	動物モデル	Male Sprague–Dawley rats
	投薬量	200 ng/kg
	投与方法	p.o.

参考

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カスタマーフィードバック

: Data independently produced by , , Mireia Vila Gasull University of Porto. 2011;Mireia Vila Gasull

: Data from [Data independently produced by , , Mol Cell Endocrinol, 2018, 470:1-13]

: Data from [Data independently produced by , , Inflammation, 2017, 40(6):1884-1893]

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：

VDR regulates mitochondrial function as a protective mechanism against renal tubular cell injury in diabetic rats [ Redox Biol, 2024, 70:103062]	PubMed: 38320454
Calcitriol impairs the secretion of IL-4 and IL-13 in Th2 cells via modulating VDR-Gata3-Gfi1 axis [ bioRxiv, 2024, ]	PubMed: none
In Vivo and In Vitro Evidence for an Interplay between the Glucocorticoid Receptor and the Vitamin D Receptor Signaling [ Cells, 2023, 12(18)2291]	PubMed: 37759513
In Vivo and In Vitro Evidence for an Interplay between the Glucocorticoid Receptor and the Vitamin D Receptor Signaling [ Cells, 2023, 12(18)2291]	PubMed: 37759513
Vitamin A- and D-Deficient Diets Disrupt Intestinal Antimicrobial Peptide Defense Involving Wnt and STAT5 Signaling Pathways in Mice [ Nutrients, 2023, 15(2)376]	PubMed: 36678247
Brk/PTK6 and Involucrin Expression May Predict Breast Cancer Cell Responses to Vitamin D3 [ Int J Mol Sci, 2023, 24(13)10757]	PubMed: 37445934
Brk/PTK6 and Involucrin Expression May Predict Breast Cancer Cell Responses to Vitamin D3 [ Int J Mol Sci, 2023, 24(13)10757]	PubMed: 37445934
Piscine Vitamin D Receptors Vdra/Vdrb in the Absence of Vitamin D Are Utilized by Grass Carp Reovirus for Promoting Viral Replication [ Microbiol Spectr, 2023, 11(4):e0128723]	PubMed: 37466438
Piscine Vitamin D Receptors Vdra/Vdrb in the Absence of Vitamin D Are Utilized by Grass Carp Reovirus for Promoting Viral Replication [ Microbiol Spectr, 2023, 11(4):e0128723]	PubMed: 37466438
Vitamin D3 suppresses the cholesterol homeostasis pathway in patient-derived glioma cell lines [ FEBS Open Bio, 2023, 13(9):1789-1806]	PubMed: 37489660

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。

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