Calcitriol

For research use only.

Catalog No.S1466 Synonyms: RO215535, Topitriol

22 publications

Calcitriol Chemical Structure

CAS No. 32222-06-3

Calcitriol (RO215535, Topitriol) 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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Selleck's Calcitriol has been cited by 22 publications

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Biological Activity

Description Calcitriol (RO215535, Topitriol) 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 M4HhbmN6fG:2b4jpZ:Kh[XO|YYm= M1HNZ|EzOCCq NELiV4REgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJS1RzMU[gZZN{\XO|ZXSgZZMh\GWlcnXhd4UhcW5iY3XscEBkd3WwdDDh[pRmeiBzMkCgbJJ{NCCLQ{WwQVFmNTB3IN88US=> MmPjNlI6OjZyNki=
human HOS cells NWPVbG1KTnWwY4Tpc44h[XO|YYm= NUfMOJd1OjRiaB?= MlP2RYN1cX[rdImgZZQhcHWvYX6gWmRTKGW6cILld5Nm\CCrbjDoeY1idiCKT2OgZ4VtdHNidILhcpNn\WO2ZXSge4l1cCCyR1yzMYhQ[yxicFPEUmEucF[GUjDhcoQheGiUTD3UT{Bie3Onc4Pl[EBieyCjc4Pld5Nm\CCjczD0doFve2O{aYD0bY9v[WxiYXP0bZZifGmxbjDt[YF{fXKnZDCyOEBpenNicH;zeEBqdm[nY4Tpc44h[nlibIXjbYZmemG|ZTDy[ZBwenSncjDn[Y5mKGG|c3H5MEBGSzVyPUHlMVA2KM7:TR?= NYHQc5FYOjF6OEmzN|Q>
human HOS/SF cells MX3GeY5kfGmxbjDhd5NigQ>? MmHoNlQhcA>? NX7oSnRtXHKjboPhZ5RqfmG2aX;uJI9nKF[GUj3t[YRq[XSnZDDvd5Rmd2OjbHPpckBxem:vb4TldkBqdiCqdX3hckBJV1NxU1[gZ4VtdHNiYX\0[ZIhOjRiaILzJIJ6KGy3Y3nm[ZJie2VicnXwc5J1\XJiZ3Xu[UBie3OjeTygSWM2OD1{Lk\lMVA2KM7:TR?= MVmyOFkxODd{OB?=
human PBMC Mn3TSpVv[3Srb36gZZN{[Xl? MnTuNlQhcA>? NV;6O4tvUW6qaXLpeIlwdiCxZjDMVHMucW6mdXPl[EBVVk[jbIDoZUBxem:mdXP0bY9vKGmwIHj1cYFvKFCETVOgZYZ1\XJiMkSgbJJ{KGK7IFXMTXNCNCCLQ{W9Nk46\S1yNTFOwG0> MUmxPVMxQTF3NR?=
mouse LM05e cells NWjS[|ZJWHKxbHnm[ZJifGmxbjDhd5NigQ>? M37wXlczKGh? M1XTXGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgcY92e2ViTF2wOYUh[2WubIOgZZN{\XO|ZXSgZZMh\GWlcnXhd4UhcW5iY3XscEBvfW2kZYKgZYZ1\XJiN{KgbJJ{KGK7IGfTWEBie3OjeTygTWM2OD1|ZT2wOUDPxE1? NEGxPGgzPDlyMEOzPS=>
rat osteosarcoma cells NX24[YNiTnWwY4Tpc44h[XO|YYm= MmWzTY5lfWO2aX;uJI9nKF[GUj3t[YRq[XSnZDCyOE1pgWS{b4j5cIF{\SC2cnHud4NzcXC2aX;uJIlvKHKjdDDvd5Rmd3OjcnPvcYEh[2WubIOgZpkhdHWlaX\ldoF{\SC{ZYDvdpRmeiCpZX7lJIF{e2G7LDDFSFUxRTBwMjDuUS=> NUTkUZFkOjF7MEKyN|U>
rat ROS 17/2.8 cells MlTVSpVv[3Srb36gZZN{[Xl? Mn3wNVYhcA>? NUfTOYE{SWO2aY\peJkh[XRiVlTSJIlvKHKjdDDSU3MhOTdxMj64JINmdGy|IHHzd4V{e2WmIHHzJJRz[W6|Y4LpdJRqd26jbDDhZ5RqfmG2aX;uJI9nKDJ2LXj5[JJwgHmuYYPlJIdmdmVicILvcY91\XJiYX\0[ZIhOTZiaILzJIJ6KGy3Y3nm[ZJie2VicnXwc5J1\XJiZ3Xu[UBie3OjeTygSWM2OD1yLkKgcm0> NYXqXHN{OTlzNke4PVM>
COS7 cells NVjGcWJ7TnWwY4Tpc44h[XO|YYm= MlX4NlQhcA>? M{XPUmFod26rc4SgZYN1cX[rdImgZZQhcHWvYX6gWmRTKGmwIFPPV|ch[2WubIOgZZN{\XO|ZXSgZZMhcW6mdXP0bY9vKG:oIITyZY5{[3KrcITpc45idCC2cnHud4FkfGm4YYTpc44h[W[2ZYKgNlQhcHK|IHL5JI1wfXOnIH;zeIVweG:wdHnuJIx2[2moZYLhd4UhemWyb4L0[ZIh\2WwZTDhd5NigSxiRVO1NF0xNjVibl2= M3HlUFE4QTB2M{ew
mouse SVEC cells M3TwZXBzd2yrZnXyZZRqd25iYYPzZZk> M4m2fVczKGh? M1jGVWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgcY92e2ViU2\FR{Bk\WyuczDhd5Nme3OnZDDhd{Bl\WO{ZXHz[UBqdiClZXzsJI52dWKncjDh[pRmeiB5MjDodpMh[nliV2PUJIF{e2G7LDDJR|UxRTBwNUKgcm0> Mnu1NlQ6ODB|M{m=
CV1 cells M2rLO2Z2dmO2aX;uJIF{e2G7 NWmxWIVXSWO2aY\peJkhd25iaIXtZY4hXkSULX3l[IlifGWmIITyZY5{[3KrcITpc44hd2Zib4P0[Y9k[WylaX6gWmRTTSCodYPl[EB1dyC2aIntbYRqdmVia3nuZZNmKHC{b33veIVzN2e{b4f0bEBpd3Kvb37lJJJmeG:{dHXyJIdmdmViaX6gR3YyKGOnbHzzMEBGTDVyPUCuO{BvVQ>? M{HUZ|E4OTR7OEiw
COS1 cells NWns[VFlTnWwY4Tpc44h[XO|YYm= NV3aeHE5TGm|cHzhZ4Vu\W62IH;mJFEu[WyyaHGsJFI2NSiRSDnbN2heTDNiZoLvcUBpfW2jbjDWSHIh\XiycnXzd4VlKGmwIFPPV|Eh[2WubIOsJGlEPTB;MD64JI5O NFLUZmEyPzl{NE[xOi=>
human PBMC MkfQSpVv[3Srb36gZZN{[Xl? NYe0SHp2OjRiaB?= MYrJcohq[mm2aX;uJI9nKEySUz3pcoR2[2WmIFnMNVIwOjOyNECgdJJw\HWldHnvckBqdiCqdX3hckBRSk2FIHHmeIVzKDJ2IHjyd{BjgSCHTFnTRUwhUUN3ME2xJI5O MojnNVk{ODlzNUW=
HEK293 cells Mm\jSpVv[3Srb36gZZN{[Xl? MnztNlQhcA>? Mke2RYdwdmm|dDDhZ5Rqfmm2eTDheEBpfW2jbjDWSHIhcW5iSFXLNlk{KGOnbHzzJIF{e2W|c3XkJIF{KGmwZIXjeIlwdiCxZjD0doFve2O{aYD0bY9v[WxidILhcpNi[3SrdnH0bY9vKGGodHXyJFI1KGi{czDifUBud3W|ZTDvd5Rmd3CxboTpckBtfWOrZnXyZZNmKHKncH;yeIVzKGenbnWgZZN{[XluIFXDOVA:OSCwTR?= MVGxO|kxPDN5MB?=
human HL60 cells NWnjR3NsTnWwY4Tpc44h[XO|YYm= NHLUPXVKdmS3Y4Tpc44hd2ZiaIXtZY4hUEx4MDDkbYZn\XKnboTpZZRqd25iYYPz[ZN{\WRiYYOgZ4VtdHNicnXkeYNqdmdibnn0do8h[my3ZTD0[ZRz[XqxbHn1cUwhTUR3ME2xJI5O MWCyNVkxOjJ|NR?=
human HeLa cells NF72WVZHfW6ldHnvckBie3OjeR?= NH;ZNYEyPiCq Mnj0WJJidnOjY4TpeoF1cW:wIH;mJGdCVDRvZoXz[YQhXkSUIHzp[4Fv\CCkaX7kbY5oKGSxbXHpckBmgHC{ZYPz[YQhcW5iaIXtZY4hUGWOYTDj[YxteyCjZoTldkAyPiCqcoOgZpkhdHWlaX\ldoF{\SC{ZYDvdpRmeiCpZX7lJIF{e2G7LDDFR|UxRTFibl2= NGXWSHczOjl3N{izOC=>
human T47D cells NYr0NXVuWHKxbHnm[ZJifGmxbjDhd5NigQ>? NWDkenQ5PzJiaB?= M2DD[2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iVES3SEBk\WyuczDhd5Nme3OnZDDhd{Bl\WO{ZXHz[UBqdiClZXzsJI52dWKncjDh[pRmeiB5MjDodpMh[nliV2PUJIF{e2G7LDDJR|UxRTFwMzDuUS=> NGfySIwzPDlyMEOzPS=>
human peripheral blood mononuclear cells MUfQdo9tcW[ncnH0bY9vKGG|c3H5 NWTXNWxTUW5idnn0do8hcW6qaXLpeIlwdiCxZjDwbJl1d2inbXHn[4x2fGmwaX7pck1qdmS3Y3XkJJN1cW23bHH0bY9vKG:oIHj1cYFvKHCncnnwbIVz[WxiYnzvc4QhdW:wb371Z4xm[XJiY3XscJMheHKxbHnm[ZJifGmxbjygSWQ2OD1{Lkegcm0> M4DOOFEyODByMEG0
human Caco-2 cells MmjvSpVv[3Srb36gZZN{[Xl? M33IbGVn\mWldDDvckBXTFJidILhcpNkemmydHnvcoFtKGGldHn2bZR6KGmwIHj1cYFvKEOjY3:tNkBk\WyuczDpckBxemW|ZX7j[UBw\iB3JTDm[ZRidCClYXzmJJNmenWvLDDFR|UxRTNwNUKgcm0> NV\QOI1oOThyNUSyN|A>
human MCF7 cells NXvGcXhyTnWwY4Tpc44h[XO|YYm= NH3od4tC\2:waYP0JIFkfGm4aYT5JIF1KHqnYoLh[ol{cCCpYXy0MXZFWiCOQlSg[ZhxemW|c3XkJIlvKGi3bXHuJG1ETjdiY3XscJMh[nlibIXjbYZmemG|ZTDy[ZBwenSncjDn[Y5mKGKjc3XkJJRz[W6|YXP0bZZifGmxbjDhd5NigSxiRVO1NF02NjVibl2= MWWyNlE5ODh|Nx?=
human THP1 cells M4fjUGZ2dmO2aX;uJIF{e2G7 M{j2WmFkfGm4YYTpc44hd2ZiVlTSJIlvKGi3bXHuJHRJWDFiY3XscJMh[XO|ZYPz[YQh[XNiaX7jdoVie2ViaX6gZ4F1cGWuaXPp[IlvKGGwdHntbYNzd2KrYXygdIVxfGmmZTDtVm5CKGW6cILld5Nqd25iYomgVnQuWEOULDDFR|UxRTFyIH7N NWj0TnN5OTl|MEmxOVU>
human HaCaT cells M4jP[mZ2dmO2aX;uJIF{e2G7 NI\nOHEzPCCq MYXUdoFve2GldHn2ZZRqd25ib3[gWmRTKGmwIHj1cYFvKEijQ3HUJINmdGy|IHHmeIVzKDJ2IHjyd{BjgSCudXPp[oVz[XOnIILldI9zfGW{IHflcoUh[XO|YYmsJGVEPTB;MD6zNlE2KM7:TR?= Mk[0NlY{PjdyMUm=
human HN12 cells MnG0VJJwdGmoZYLheIlwdiCjc4PhfS=> M1fU[lczKGh? MnPURY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKTkGyJINmdGy|IHHzd4V{e2WmIHHzJIRm[3KnYYPlJIlvKGOnbHygcpVu[mW{IHHmeIVzKDd{IHjyd{BjgSCZU2SgZZN{[XluIFnDOVA:OC53NUOg{txO NHHITIszPDlyMEOzPS=>
human HaCaT cells NYnvbWFsTnWwY4Tpc44h[XO|YYm= NW\kRYpxUW6qaXLpeIlwdiCxZjDjc4xwdnliZn;ycYF1cW:wIH;mJIh2dWGwIFjhR4FVKGOnbHzz NVHKeFlOOjJ2MESzNlY>
human HCT116 cells NHzMRolHfW6ldHnvckBie3OjeR?= Mlj0NlAuPDBizszN M17OZVI1KGh? MkP3RYdwdmm|dDDhZ5Rqfmm2eTDheEBTSVJiKIXub45wf25ib4Lp[4lvMSCneIDy[ZN{\WRiaX6gbJVu[W5iSFPUNVE3KGOnbHzzJINwNWW6cILld5NqdmdiUlHSSUBifCB{MDD0c{A1OCC3TTDh[pRmeiB{NDDodpMh[nlibIXjbYZmemG|ZTDy[ZBwenSncjDn[Y5mKGG|c3H5 NYX2eHp3OjN{N{[0OFk>
mouse C3H10T1/2 cells MX\GeY5kfGmxbjDhd5NigQ>? MVOwMlUuPSEQvF2= NXvWWVg5OjRiaB?= NX3OVGNDUW6qaXLpeIlwdiCxZjDI[YRo\WixZzDzbYdv[WyrbnegdIF1cHejeTDpckBud3W|ZTDDN2gyOFRzL{KgZ4VtdHNiYYPz[ZN{\WRiYYOg[I94diC{ZXf1cIF1cW:wIH;mJGdtcTFiYYSgNE42KHSxIEWgeW0h[W[2ZYKgNlQhcHK|IHL5JHJVNVCFUjDhcoFtgXOrcx?= NHzKRVMzOjJ{Nk[1Oy=>
human A498 cells NE\RNXFHfW6ldHnvckBie3OjeR?= M4rNN|AvODFizszN MofqOEBp NYL2NJpNUW6mdXP0bY9vKG:oIFPZVFI1KG2UTlGg[ZhxemW|c3nvckBqdiCqdX3hckBCPDl6IHPlcIx{KGG2IECuNFEh|ryPIHHmeIVzKDRiaILzJIJ6KFKWLWDDVkBidmGueYPpdy=> MkXVNlE{QTJ7OEO=

... 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)
Water Insoluble
Ethanol '83 mg/mL

* 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
Smiles CC(CCCC(C)(C)O)C1CCC2C1(CCCC2=CC=C3CC(CC(C3=C)O)O)C

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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