Calcitriol | 钙三醇 | 1,25-Dihydroxyvitamin D3 | VDR Agonist

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Calcitriol/骨化三醇 {[allProObj[0].p_purity_real_show]}

货号：A132740 同义名： 钙三醇 / 1,25-Dihydroxyvitamin D3; 1α,25-dihydroxy Vitamin D3

Calcitriol 是维生素 D3 的活性形式，对维生素 D 受体（VDR）具有高亲和力，IC50 值为 1 nM。Calcitriol 具有调节钙磷代谢、抗炎和抗肿瘤作用，可用于骨质疏松症、慢性肾病和癌症的研究。

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Type	HazMat fee for 500 gram (Estimated)
Excepted Quantity	USD 0.00
Limited Quantity	USD 15-60
Inaccessible (Haz class 6.1), Domestic	USD 80+
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Accessible (Haz class 3, 4, 5 or 8), International	USD 200+

Calcitriol/骨化三醇化学结构
CAS号：32222-06-3

Calcitriol/骨化三醇 3D分子结构
CAS号：32222-06-3

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Calcitriol/骨化三醇纯度/质量文件产品仅供科研

货号：A132740 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

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Calcitriol/骨化三醇生物活性

描述

VDR (vitamin D receptor), as a member of the nuclear receptor superfamily, mediates the biological activity of 1,25-dihydroxyvitamin D3 (calcitriol) which is generated from vitamin D by successive hydroxylations in the liver and kidney. VDR can regulate a variety of illnesses in intestine, kidney, bone, skin, heart, and various other organs^[3]. Calcitriol, the most biologically active metabolite of vitamin D, is a non-selective VDR agonist with IC₅₀ of 0.4 nM. Calcitriol is a potent inhibitor of PHA (phytohemagglutinin)-induced lymphocyte proliferation, achieving 70% inhibition of tritiated thymidine incorporation after 72 h in culture. Furthermore, calcitriol suppresses interleukin-2 (IL-2) production by PHA-stimulated peripheral blood mononuclear cells in a concentration-dependent fashion^[4]. In HL-60 cells, a human myelomonocytic leukemia cell line, calcitriol arrests cells in G1; this effect is mediated through an increase in p27. Calcitriol mediated arrest in G0/G1 is also observed in human breastcancer lines. In vivo, a decrease in tumor volume induced by calcitriol correlates with a significant decrease in the intratumoral p21 expression^[5].

Calcitriol/骨化三醇细胞研究

细胞系	浓度	检测类型	检测时间	活性说明	数据源
COS1 cells		Function assay		Displacement of 1-alpha, 25-(OH)[3H]D3 from human VDR expressed in COS1 cells, IC50=0.8 nM	17924616
COS7 cells		Function assay	24 h	Agonist activity at human VDR in COS7 cells assessed as induction of transcriptional transactivation after 24 hrs by mouse osteopontin luciferase reporter gene assay, EC50=0.5 nM	17904370
CV1 cells		Function assay		Activity on human VDR-mediated transcription of osteocalcin VDRE fused to thymidine kinase promoter/growth hormone reporter gene in CV1 cells, ED50=0.7 nM	17149880
HEK293 cells		Function assay	24 h	Agonist activity at human VDR in HEK293 cells assessed as induction of transcriptional transactivation after 24 hrs by mouse osteopontin luciferase reporter gene assay, EC50=1 nM	17904370

Calcitriol/骨化三醇参考文献

[1]24(9):876-887.

[2]74(4):1451-1455.

[3]Shang M, Sun J. Vitamin D/VDR, Probiotics, and Gastrointestinal Diseases. Curr Med Chem. 2017;24(9):876-887.

Calcitriol/骨化三醇实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.40mL

0.48mL

0.24mL

12.00mL

2.40mL

1.20mL

24.00mL

4.80mL

2.40mL

Calcitriol/骨化三醇技术信息

CAS号	32222-06-3
分子式	C₂₇H₄₄O₃
分子量	416.64
SMILES Code	C[C@@]12[C@](CC[C@]2([H])[C@H](C)CCCC(C)(O)C)([H])/C(CCC1)=C/C=C3C([C@H](C[C@@H](C\3)O)O)=C
MDL No.	MFCD00867079

别名	钙三醇 ;1,25-Dihydroxyvitamin D3; 1α,25-dihydroxy Vitamin D3; 1,25(OH)2D; 1α,25-(OH)2D3; 1,25-dihydroxycholecalciferol; Soltriol; Silkis; Topitriol; Calcijex; Rocaltrol
运输	蓝冰

存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Inert atmosphere, store in freezer, under -20°C

溶解方案

细胞实验：

DMSO: 105 mg/mL(252.02 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

无水乙醇: 100 mg/mL(240.02 mM)，配合低频超声助溶，注意：无水乙醇开封后，易挥发，也会吸收空气中的水分，导致溶解能力下降，请避免使用开封较久的乙醇

动物实验：请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用；以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

方案一

方案二

细胞研究

细胞系	浓度	检测类型	检测时间	活性说明	数据源

COS1 cells		Function assay		Displacement of 1-alpha, 25-(OH)[3H]D3 from human VDR expressed in COS1 cells, IC50=0.8 nM	17924616
COS7 cells		Function assay	24 h	Agonist activity at human VDR in COS7 cells assessed as induction of transcriptional transactivation after 24 hrs by mouse osteopontin luciferase reporter gene assay, EC50=0.5 nM	17904370
CV1 cells		Function assay		Activity on human VDR-mediated transcription of osteocalcin VDRE fused to thymidine kinase promoter/growth hormone reporter gene in CV1 cells, ED50=0.7 nM	17149880
HEK293 cells		Function assay	24 h	Agonist activity at human VDR in HEK293 cells assessed as induction of transcriptional transactivation after 24 hrs by mouse osteopontin luciferase reporter gene assay, EC50=1 nM	17904370
human A498 cells	0.01 μM	Function assay	4 h	Induction of CYP24 mRNA expression in human A498 cells at 0.01 μM after 4 hrs by RT-PCR analysis	21392983
human Caco-2 cells		Function assay		Effect on VDR transcriptional activity in human Caco-2 cells in presence of 5% fetal calf serum, EC50=3.52 nM	18054230
human HaCaT cells		Function assay	24 h	Transactivation of VDR in human HaCaT cells after 24 hrs by luciferase reporter gene assay, EC50=0.3215 μM	26367019
human HaCaT cells		Function assay		Inhibition of colony formation of human HaCaT cells	22404326
human HCT116		Cytotoxic assay	120 h	Cytotoxicity against human HCT116 assessed as decrease in cell count after 120 hrs, IC50=1e-05 μM	22926068
human HCT116 cells	20-40 μM	Function assay	24 h	Agonist activity at RAR (unknown origin) expressed in human HCT116 cells co-expressing RARE at 20 to 40 uM after 24 hrs by luciferase reporter gene assay	23276449
human HeLa cells		Function assay	16 h	Transactivation of GAL4-fused VDR ligand binding domain expressed in human HeLa cells after 16 hrs by luciferase reporter gene assay, EC50=1 nM	22957834
human HL60 cells		Function assay		Induction of human HL60 differentiation assessed as cells reducing nitro blue tetrazolium, ED50=1 nM	21902235
human HN12 cells		Proliferation assay	72 h	Antiproliferative activity against human HN12 cells assessed as decrease in cell number after 72 hrs by WST assay, IC50=0.553 μM	24900339
human HOS cells		Function assay	24 h	Activity at human VDR expressed in human HOS cells transfected with pGL3-hOc, pCDNA-hVDR and phRL-TK assessed as assessed as transcriptional activation measured 24 hrs post infection by luciferase reporter gene assay, EC50=1e-05 μM	21889334
human HOS/SF cells		Function assay	24 h	Transactivation of VDR-mediated osteocalcin promoter in human HOS/SF cells after 24 hrs by luciferase reporter gene assay, EC50=2.6e-05 μM	24900728
human MCF7 cells		Function assay		Agonist activity at zebrafish gal4-VDR LBD expressed in human MCF7 cells by luciferase reporter gene based transactivation assay, EC50=5.5 nM	22180837
human PBMC		Function assay	24 h	Inhibition of LPS-induced TNFalpha production in human PBMC after 24 hrs by ELISA, IC5=2.9e-05 μM	19309155
human PBMC		Function assay	24 h	Inhibition of LPS-induced IL12/23p40 production in human PBMC after 24 hrs by ELISA, IC50=1 nM	19309155
human peripheral blood mononuclear cells		Proliferation assay		In vitro inhibition of phytohemagglutininin-induced stimulation of human peripheral blood mononuclear cells proliferation, ED50=2.7 nM	11000014
human T47D cells		Proliferation assay	72 h	Antiproliferative activity against human T47D cells assessed as decrease in cell number after 72 hrs by WST assay, IC50=1.3 nM	24900339
human THP1 cells		Function assay		Activation of VDR in human THP1 cells assessed as increase in cathelicidin antimicrobial peptide mRNA expression by RT-PCR, EC50=10 nM	19309155
mouse C3H10T1/2 cells	0.5-5 μM	Function assay	24 h	Inhibition of Hedgehog signaling pathway in mouse C3H10T1/2 cells assessed as down regulation of Gli1 at 0.5 to 5 uM after 24 hrs by RT-PCR analysis	22226657
mouse LM05e cells		Proliferation assay	72 h	Antiproliferative activity against mouse LM05e cells assessed as decrease in cell number after 72 hrs by WST assay, IC50=3e-05 μM	24900339
mouse SVEC cells		Proliferation assay	72 h	Antiproliferative activity against mouse SVEC cells assessed as decrease in cell number after 72 hrs by WST assay, IC50=0.52 nM	24900339
rat osteosarcoma cells		Function assay		Induction of VDR-mediated 24-hydroxylase transcription in rat osteosarcoma cells by luciferase reporter gene assay, ED50=0.2 nM	21902235
rat ROS 17/2.8 cells		Function assay	16 h	Activity at VDR in rat ROS 17/2.8 cells assessed as transcriptional activation of 24-hydroxylase gene promoter after 16 hrs by luciferase reporter gene assay, EC50=0.2 nM	19167893

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最近浏览的产品

大规格询价

摩尔计算器

靶点

总药量计算器

工作液计算器

细胞研究

临床研究

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Calcitriol/骨化三醇纯度/质量文件产品仅供科研

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Calcitriol/骨化三醇细胞研究

Calcitriol/骨化三醇参考文献

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