Calcitriol

Catalog No.S1466 Synonyms: RO215535, Topitriol

Calcitriol Chemical Structure

Molecular Weight(MW): 416.64

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.

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In DMSO USD 500 In stock
USD 120 In stock
USD 270 In stock
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Cited by 10 Publications

3 Customer Reviews

  • Mireia Vila Gasull University of Porto. 2011;Mireia Vila Gasull . Calcitriol purchased from Selleck.

    To chemically induce klotho expression, THP-1 cells were treated with Calcitriol. The effects were evaluated on the gene level with real time PCR from 5 to 480 min after treatment and on the protein level with western blot after 48 h and 72 h.

    Mol Cell Endocrinol, 2018, 470:1-13. Calcitriol purchased from Selleck.

  • Calcitriol alleviates inflammation in vivo accompanied by upregulated A20. c HE staining, CD3+ lymphocyte and F4/80+ macrophage staining. Values are shown as mean ± SD, n = 5 per group. **P < 0.01 among groups. ΔΔP < 0.01 versus control.

    Inflammation, 2017, 40(6):1884-1893. Calcitriol purchased from Selleck.

Purity & Quality Control

Choose Selective Vitamin Inhibitors

Biological Activity

Description 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.
Targets
vitamin D receptor [1]
(Cell-free assay)
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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human HCT116 M124eGN6fG:2b4jpZ:Kh[XO|YYm= NXzXclZpOTJyIHi= M2TVSGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGhEXDFzNjDhd5Nme3OnZDDhd{Bl\WO{ZXHz[UBqdiClZXzsJINwfW62IHHmeIVzKDF{MDDodpMtKEmFNUC9NYUuODVizszN NFfhUoozOjl{NkC2PC=>
human HOS cells NFXRbmtHfW6ldHnvckBie3OjeR?= MmT2NlQhcA>? NYLNSWRwSWO2aY\peJkh[XRiaIXtZY4hXkSUIHX4dJJme3OnZDDpckBpfW2jbjDIU3Mh[2WubIOgeJJidnOoZXP0[YQhf2m2aDDwS2w{NWiRYzygdGNFVkFvaG\EVkBidmRicHjSUE1VUyCjc4Pld5Nm\CCjczDhd5Nme3OnZDDhd{B1emGwc3PybZB1cW:wYXygZYN1cX[jdHnvckBu\WG|dYLl[EAzPCCqcoOgdI9{fCCrbn\lZ5Rqd25iYomgcJVkcW[ncnHz[UBz\XCxcoTldkBo\W6nIHHzd4F6NCCHQ{WwQVFmNTB3IN88US=> NHvYd48zOTh6OUOzOC=>
human HOS/SF cells NHPQRndHfW6ldHnvckBie3OjeR?= M1LJZlI1KGh? MmTMWJJidnOjY4TpeoF1cW:wIH;mJHZFWi2vZXTpZZRm\CCxc4Tlc4NidGOrbjDwdo9ud3SncjDpckBpfW2jbjDIU3MwW0ZiY3XscJMh[W[2ZYKgNlQhcHK|IHL5JIx2[2moZYLhd4UhemWyb4L0[ZIh\2WwZTDhd5NigSxiRVO1NF0zNj[nLUC1JO69VQ>? NIH2UmszPDlyMEeyPC=>
human PBMC NEfjR3lHfW6ldHnvckBie3OjeR?= M{nkXlI1KGh? M3z4WmlvcGmkaYTpc44hd2ZiTGDTMYlv\HWlZXSgWG5H[WyyaHGgdJJw\HWldHnvckBqdiCqdX3hckBRSk2FIHHmeIVzKDJ2IHjyd{BjgSCHTFnTRUwhUUN3PUKuPYUuODVizszN M4G4[|E6OzB7MUW1
mouse LM05e cells MV7Qdo9tcW[ncnH0bY9vKGG|c3H5 NEOyWnc4OiCq NH;yT41CdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JI1wfXOnIFzNNFVmKGOnbHzzJIF{e2W|c3XkJIF{KGSnY4LlZZNmKGmwIHPlcIwhdnWvYnXyJIFnfGW{IEeyJIhzeyCkeTDXV3Qh[XO|YYmsJGlEPTB;M3WtNFUh|ryP M3TYVlI1QTByM{O5
rat osteosarcoma cells NH\SOJNHfW6ldHnvckBie3OjeR?= M4fE[Wlv\HWldHnvckBw\iCYRGKtcYVlcWG2ZXSgNlQucHmmcn;4fYxie2VidILhcpNkemmydHnvckBqdiC{YYSgc5N1\W:|YYLjc41iKGOnbHzzJIJ6KGy3Y3nm[ZJie2VicnXwc5J1\XJiZ3Xu[UBie3OjeTygSWQ2OD1yLkKgcm0> NFHQTZozOTlyMkKzOS=>
rat ROS 17/2.8 cells M1u4RmZ2dmO2aX;uJIF{e2G7 NFS1XYYyPiCq NEL3XHFC[3Srdnn0fUBifCCYRGKgbY4hemG2IGLPV{AyPy9{LkigZ4VtdHNiYYPz[ZN{\WRiYYOgeJJidnOlcnnweIlwdmGuIHHjeIl3[XSrb36gc4YhOjRvaInkdo95gWyjc3Wg[4Vv\SCycn;tc5RmeiCjZoTldkAyPiCqcoOgZpkhdHWlaX\ldoF{\SC{ZYDvdpRmeiCpZX7lJIF{e2G7LDDFR|UxRTBwMjDuUS=> MUKxPVE3Pzh7Mx?=
COS7 cells MkPQSpVv[3Srb36gZZN{[Xl? MX:yOEBp NFHRXHRC\2:waYP0JIFkfGm4aYT5JIF1KGi3bXHuJHZFWiCrbjDDU3M4KGOnbHzzJIF{e2W|c3XkJIF{KGmwZIXjeIlwdiCxZjD0doFve2O{aYD0bY9v[WxidILhcpNi[3SrdnH0bY9vKGGodHXyJFI1KGi{czDifUBud3W|ZTDvd5Rmd3CxboTpckBtfWOrZnXyZZNmKHKncH;yeIVzKGenbnWgZZN{[XluIFXDOVA:OC53IH7N NYO0VVhiOTd7MESzO|A>
mouse SVEC cells MoC4VJJwdGmoZYLheIlwdiCjc4PhfS=> MnLDO|IhcA>? NFHkPJpCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JI1wfXOnIGPWSWMh[2WubIOgZZN{\XO|ZXSgZZMh\GWlcnXhd4UhcW5iY3XscEBvfW2kZYKgZYZ1\XJiN{KgbJJ{KGK7IGfTWEBie3OjeTygTWM2OD1yLkWyJI5O NGHmT4gzPDlyMEOzPS=>
CV1 cells M1\nZ2Z2dmO2aX;uJIF{e2G7 NGC0WoVC[3Srdnn0fUBwdiCqdX3hckBXTFJvbXXkbYF1\WRidILhcpNkemmydHnvckBw\iCxc4Tlc4NidGOrbjDWSHJGKG[3c3XkJJRwKHSqeX3p[Ilv\SCtaX7hd4UheHKxbX;0[ZIw\3Kxd4ToJIhwem2xbnWgdoVxd3K2ZYKg[4Vv\SCrbjDDWlEh[2WubIOsJGVFPTB;MD63JI5O NXTrT|I4OTdzNEm4PFA>
COS1 cells NYS0SnJOTnWwY4Tpc44h[XO|YYm= M1\LO2Rqe3CuYXPlcYVvfCCxZjCxMYFteGijLDCyOU0pV0hrW{PIYWQ{KG[{b32gbJVu[W5iVlTSJIV5eHKnc4Pl[EBqdiCFT2OxJINmdGy|LDDJR|UxRTBwODDuUS=> NWjBcWJyOTd7MkS2NVY>
human PBMC MYXGeY5kfGmxbjDhd5NigQ>? MYGyOEBp NGHwVHlKdmirYnn0bY9vKG:oIFzQV{1qdmS3Y3XkJGlNOTJxMkPwOFAheHKxZIXjeIlwdiCrbjDoeY1idiCSQl3DJIFnfGW{IEK0JIhzeyCkeTDFUGlUSSxiSVO1NF0yKG6P MkfzNVk{ODlzNUW=
HEK293 cells NXrVUG9yTnWwY4Tpc44h[XO|YYm= NUC5bGFkOjRiaB?= Mn[2RYdwdmm|dDDhZ5Rqfmm2eTDheEBpfW2jbjDWSHIhcW5iSFXLNlk{KGOnbHzzJIF{e2W|c3XkJIF{KGmwZIXjeIlwdiCxZjD0doFve2O{aYD0bY9v[WxidILhcpNi[3SrdnH0bY9vKGGodHXyJFI1KGi{czDifUBud3W|ZTDvd5Rmd3CxboTpckBtfWOrZnXyZZNmKHKncH;yeIVzKGenbnWgZZN{[XluIFXDOVA:OSCwTR?= NXT3V5FwOTd7MESzO|A>
human HL60 cells MVXGeY5kfGmxbjDhd5NigQ>? M37KXGlv\HWldHnvckBw\iCqdX3hckBJVDZyIHTp[oZmemWwdHnheIlwdiCjc4Pld5Nm\CCjczDj[YxteyC{ZXT1Z4lv\yCwaYTyc{BjdHWnIITleJJigm:uaYXtMEBGTDVyPUGgcm0> MXyyNVkxOjJ|NR?=
human HeLa cells MVXGeY5kfGmxbjDhd5NigQ>? NX\X[mJMOTZiaB?= MXHUdoFve2GldHn2ZZRqd25ib3[gS2FNPC2odYPl[EBXTFJibHnnZY5lKGKrbnTpcoch\G:vYXnuJIV5eHKnc4Pl[EBqdiCqdX3hckBJ\UyjIHPlcIx{KGGodHXyJFE3KGi{czDifUBtfWOrZnXyZZNmKHKncH;yeIVzKGenbnWgZZN{[XluIFXDOVA:OSCwTR?= NILldVUzOjl3N{izOC=>
human T47D cells MoHNVJJwdGmoZYLheIlwdiCjc4PhfS=> MnXBO|IhcA>? MV\BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFR2N1SgZ4VtdHNiYYPz[ZN{\WRiYYOg[IVkemWjc3WgbY4h[2WubDDueY1j\XJiYX\0[ZIhPzJiaILzJIJ6KFeVVDDhd5NigSxiSVO1NF0yNjNibl2= NH7hNJEzPDlyMEOzPS=>
human peripheral blood mononuclear cells MkXqVJJwdGmoZYLheIlwdiCjc4PhfS=> M3ftdWlvKH[rdILvJIlvcGmkaYTpc44hd2ZicHj5eI9p\W2jZ3fseZRqdmmwaX6tbY5lfWOnZDDzeIlufWyjdHnvckBw\iCqdX3hckBx\XKrcHjldoFtKGKub3;kJI1wdm:wdXPs[YFzKGOnbHzzJJBzd2yrZnXyZZRqd25uIFXEOVA:Oi55IH7N MXuxNVAxODBzNB?=
human Caco-2 cells NUfLV3FRTnWwY4Tpc44h[XO|YYm= NVLkNmYzTW[oZXP0JI9vKF[GUjD0doFve2O{aYD0bY9v[WxiYXP0bZZqfHliaX6gbJVu[W5iQ3Hjc{0zKGOnbHzzJIlvKHC{ZYPlcoNmKG:oIEWlJIZmfGGuIHPhcIYhe2W{dX2sJGVEPTB;Mz61NkBvVQ>? MYixPFA2PDJ|MB?=
human MCF7 cells MWTGeY5kfGmxbjDhd5NigQ>? MkjtRYdwdmm|dDDhZ5Rqfmm2eTDheEB7\WK{YX\pd4gh\2GuND3WSHIhVEKGIHX4dJJme3OnZDDpckBpfW2jbjDNR2Y4KGOnbHzzJIJ6KGy3Y3nm[ZJie2VicnXwc5J1\XJiZ3Xu[UBj[XOnZDD0doFve2GldHn2ZZRqd25iYYPzZZktKEWFNUC9OU42KG6P NIHhfm4zOjF6MEizOy=>
human THP1 cells NX3YOHh1TnWwY4Tpc44h[XO|YYm= M2jk[2FkfGm4YYTpc44hd2ZiVlTSJIlvKGi3bXHuJHRJWDFiY3XscJMh[XO|ZYPz[YQh[XNiaX7jdoVie2ViaX6gZ4F1cGWuaXPp[IlvKGGwdHntbYNzd2KrYXygdIVxfGmmZTDtVm5CKGW6cILld5Nqd25iYomgVnQuWEOULDDFR|UxRTFyIH7N NX3NXIJxOTl|MEmxOVU>
human HaCaT cells Mlu1SpVv[3Srb36gZZN{[Xl? MYKyOEBp NVrrTFRkXHKjboPhZ5RqfmG2aX;uJI9nKF[GUjDpckBpfW2jbjDIZWNiXCClZXzsd{Bi\nSncjCyOEBpenNiYomgcJVkcW[ncnHz[UBz\XCxcoTldkBo\W6nIHHzd4F6NCCHQ{WwQVAvOzJzNTFOwG0> Mn3INlY{PjdyMUm=
human HN12 cells NVnudZBjWHKxbHnm[ZJifGmxbjDhd5NigQ>? Mn;OO|IhcA>? MoW3RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKTkGyJINmdGy|IHHzd4V{e2WmIHHzJIRm[3KnYYPlJIlvKGOnbHygcpVu[mW{IHHmeIVzKDd{IHjyd{BjgSCZU2SgZZN{[XluIFnDOVA:OC53NUOg{txO NILo[YYzPDlyMEOzPS=>
human HaCaT cells MkXsSpVv[3Srb36gZZN{[Xl? NFq2THNKdmirYnn0bY9vKG:oIHPvcI9vgSCob4LtZZRqd25ib3[gbJVu[W5iSHHDZXQh[2WubIO= NX7JWZhQOjJ2MESzNlY>
human HCT116 cells NWnKUHZWTnWwY4Tpc44h[XO|YYm= M2\odVIxNTRyIN88US=> Ml3oNlQhcA>? MnjERYdwdmm|dDDhZ5Rqfmm2eTDheEBTSVJiKIXub45wf25ib4Lp[4lvMSCneIDy[ZN{\WRiaX6gbJVu[W5iSFPUNVE3KGOnbHzzJINwNWW6cILld5NqdmdiUlHSSUBifCB{MDD0c{A1OCC3TTDh[pRmeiB{NDDodpMh[nlibIXjbYZmemG|ZTDy[ZBwenSncjDn[Y5mKGG|c3H5 NHOxNJYzOzJ5NkS0PS=>
mouse C3H10T1/2 cells M3G2R2Z2dmO2aX;uJIF{e2G7 Ml65NE42NTVizszN NIDrbVYzPCCq MlL1TY5pcWKrdHnvckBw\iCKZXTn[Yhw\yC|aXfuZYxqdmdicHH0bJdigSCrbjDtc5V{\SCFM1ixNHQyNzJiY3XscJMh[XO|ZYPz[YQh[XNiZH;3ckBz\We3bHH0bY9vKG:oIFfsbVEh[XRiMD61JJRwKDVidV2gZYZ1\XJiMkSgbJJ{KGK7IGLUMXBEWiCjbnHsfZNqew>? NG\NR|gzOjJ{Nk[1Oy=>
human A498 cells MYHGeY5kfGmxbjDhd5NigQ>? NYjQT|N1OC5yMTFOwG0> NX;IUJJHPCCq MljlTY5lfWO2aX;uJI9nKEO\UEK0JI1TVkFiZYjwdoV{e2mxbjDpckBpfW2jbjDBOFk5KGOnbHzzJIF1KDBwMEGg{txOKGGodHXyJFQhcHK|IHL5JHJVNVCFUjDhcoFtgXOrcx?= MVGyNVM6Ojl6Mx?=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
CyclinD1 ; 

PubMed: 28643892     


Immunoblot analysis of cyclinD1 in AXT cells treated with the indicated concentrations of calcitriol for 14 h. 

IRE1α / p-eIF2α / eIF2α / Atf4 / CHOP ; 

PubMed: 28643892     


Immunoblot analysis of Ire1a and total or phosphorylated (p-) forms of eIf2a, Atf4 and Chop in AXT cells treated with 5 lM calcitriol for the indicated times.

p-PERK / PERK ; 

PubMed: 28643892     


Immunoblot analysis of total or phosphorylated (p-) forms of Perk and Atf4 in AXT cells treated with 5 lM calcitriol for the indicated times or with 1 lM thapsigardin (Thap) for 1.5 h.

FGFR1 / FGFR2 / FGFR3 / FGFR4 ; 

PubMed: 29776409     


Representative immunoblots and average data (n = 6) of FGFR1, FGFR2, FGFR3, and FGFR4 from control and calcitriol (1 and 10 nM)-treated HL-1 cells.

Wnt10b / Wnt16 ; 

PubMed: 30149605     


Wnt10b and Wnt 16 protein expression in calcitriol-treated osteoclasts. With calcitriol treatment of 10 to 100 nM overnight, Western blot analysis showed a significant increase in Wnt 10b expression. Wnt 16 expression in osteoclasts after different doses of calcitriol was not significantly different at the protein level. Actin protein served as a loading control. 

28643892 29776409 30149605

Protocol

Solubility (25°C)

In vitro DMSO 83 mg/mL (199.21 mM)
Ethanol 83 mg/mL (199.21 mM)
Water 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.

Chemical Information

Molecular Weight 416.64
Formula

C27H44O3

CAS No. 32222-06-3
Storage powder
in solvent
Synonyms RO215535, Topitriol

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03029429 Recruiting Drug: Theophylline|Drug: Placebos Pseudohypoparathyroidism|Albright Hereditary Osteodystrophy Vanderbilt University Medical Center|Harvard University September 1 2018 Phase 2
NCT02714361 Completed Dietary Supplement: Vitamin D3 supplement|Other: Placebo Iron Deficiency|Anemia; Deficiency Nutritional With Poor Iron Absorption|Vitamin D Deficiency University of Chester|Medical Research Council September 2015 Not Applicable
NCT02332135 Unknown status Procedure: microwave ablation|Drug: active vitamin D Secondary Hyperparathyroidism|Maintenance Hemodialysis Wenhu Liu|Beijing Friendship Hospital January 2015 Not Applicable

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID