Calcitriol

For research use only.

Catalog No.S1466 Synonyms: RO215535, Topitriol

20 publications

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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Selleck's Calcitriol has been cited by 20 publications

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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 NUDSb5ZNS3m2b4TvfIlkyqCjc4PhfS=> NYjXXo9LOTJyIHi= Ml36R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTGNVOTF4IHHzd4V{e2WmIHHzJIRm[3KnYYPlJIlvKGOnbHygZ492dnRiYX\0[ZIhOTJyIHjyd{whUUN3ME2x[U0xPSEQvF2= NHLkb3AzOjl{NkC2PC=>
human HOS cells NILPWlJHfW6ldHnvckBie3OjeR?= Ml[xNlQhcA>? NGXCOpFC[3Srdnn0fUBifCCqdX3hckBXTFJiZYjwdoV{e2WmIHnuJIh2dWGwIFjPV{Bk\WyuczD0doFve2[nY4Tl[EB4cXSqIIDHUFMucE:lLDDwR2RPSS2qVlTSJIFv\CCyaGLMMXRMKGG|c3Xzd4VlKGG|IHHzd4V{e2WmIHHzJJRz[W6|Y4LpdJRqd26jbDDhZ5RqfmG2aX;uJI1m[XO3cnXkJFI1KGi{czDwc5N1KGmwZnXjeIlwdiCkeTDseYNq\mW{YYPlJJJmeG:{dHXyJIdmdmViYYPzZZktKEWFNUC9NYUuODVizszN M3OwXVIyQDh7M{O0
human HOS/SF cells NHPZVXVHfW6ldHnvckBie3OjeR?= NUPZTXgyOjRiaB?= NUj1eVFmXHKjboPhZ5RqfmG2aX;uJI9nKF[GUj3t[YRq[XSnZDDvd5Rmd2OjbHPpckBxem:vb4TldkBqdiCqdX3hckBJV1NxU1[gZ4VtdHNiYX\0[ZIhOjRiaILzJIJ6KGy3Y3nm[ZJie2VicnXwc5J1\XJiZ3Xu[UBie3OjeTygSWM2OD1{Lk\lMVA2KM7:TR?= NWiyVZR[OjR7MEC3Nlg>
human PBMC MnXVSpVv[3Srb36gZZN{[Xl? Mo\3NlQhcA>? MoKwTY5pcWKrdHnvckBw\iCOUGOtbY5lfWOnZDDUUmZidHCqYTDwdo9lfWO2aX;uJIlvKGi3bXHuJHBDVUNiYX\0[ZIhOjRiaILzJIJ6KEWOSWPBMEBKSzV;Mj65[U0xPSEQvF2= M3XEOFE6OzB7MUW1
mouse LM05e cells NFjwTG5Rem:uaX\ldoF1cW:wIHHzd4F6 MXy3NkBp M1jvWmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgcY92e2ViTF2wOYUh[2WubIOgZZN{\XO|ZXSgZZMh\GWlcnXhd4UhcW5iY3XscEBvfW2kZYKgZYZ1\XJiN{KgbJJ{KGK7IGfTWEBie3OjeTygTWM2OD1|ZT2wOUDPxE1? NX7Ib2hnOjR7MECzN|k>
rat osteosarcoma cells NYnPdFVOTnWwY4Tpc44h[XO|YYm= NYiwUIF2UW6mdXP0bY9vKG:oIG\EVk1u\WSrYYTl[EAzPC2qeXTyc5h6dGG|ZTD0doFve2O{aYD0bY9vKGmwIILheEBwe3Snb4PhdoNwdWFiY3XscJMh[nlibIXjbYZmemG|ZTDy[ZBwenSncjDn[Y5mKGG|c3H5MEBGTDVyPUCuNkBvVQ>? NV65fmZbOjF7MEKyN|U>
rat ROS 17/2.8 cells M2nRWmZ2dmO2aX;uJIF{e2G7 MonkNVYhcA>? MoizRYN1cX[rdImgZZQhXkSUIHnuJJJifCCUT2OgNVcwOi56IHPlcIx{KGG|c3Xzd4VlKGG|IITyZY5{[3KrcITpc45idCCjY4TpeoF1cW:wIH;mJFI1NWi7ZILvfJlt[XOnIHflcoUheHKxbX;0[ZIh[W[2ZYKgNVYhcHK|IHL5JIx2[2moZYLhd4UhemWyb4L0[ZIh\2WwZTDhd5NigSxiRVO1NF0xNjJibl2= NV\WOnFqOTlzNke4PVM>
COS7 cells MWXGeY5kfGmxbjDhd5NigQ>? NHzIe2kzPCCq M2DDe2Fod26rc4SgZYN1cX[rdImgZZQhcHWvYX6gWmRTKGmwIFPPV|ch[2WubIOgZZN{\XO|ZXSgZZMhcW6mdXP0bY9vKG:oIITyZY5{[3KrcITpc45idCC2cnHud4FkfGm4YYTpc44h[W[2ZYKgNlQhcHK|IHL5JI1wfXOnIH;zeIVweG:wdHnuJIx2[2moZYLhd4UhemWyb4L0[ZIh\2WwZTDhd5NigSxiRVO1NF0xNjVibl2= NED1eWkyPzlyNEO3NC=>
mouse SVEC cells NFrj[YhRem:uaX\ldoF1cW:wIHHzd4F6 MoT4O|IhcA>? NETPcYJCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JI1wfXOnIGPWSWMh[2WubIOgZZN{\XO|ZXSgZZMh\GWlcnXhd4UhcW5iY3XscEBvfW2kZYKgZYZ1\XJiN{KgbJJ{KGK7IGfTWEBie3OjeTygTWM2OD1yLkWyJI5O NIrVcYkzPDlyMEOzPS=>
CV1 cells M2L0WWZ2dmO2aX;uJIF{e2G7 M2D0OmFkfGm4aYT5JI9vKGi3bXHuJHZFWi2vZXTpZZRm\CC2cnHud4NzcXC2aX;uJI9nKG:|dHXvZ4Ft[2mwIG\EVmUh\nW|ZXSgeI8hfGi7bXnkbY5mKGurbnHz[UBxem:vb4Tldk9oem:5dHigbI9zdW:wZTDy[ZBwenSncjDn[Y5mKGmwIFPWNUBk\WyuczygSWQ2OD1yLkegcm0> NFH6R|kyPzF2OUi4NC=>
COS1 cells NWTm[G9HTnWwY4Tpc44h[XO|YYm= NHL6c4hFcXOybHHj[Y1mdnRib3[gNU1idHCqYTygNlUuME:KKWuzTH1FOyCocn;tJIh2dWGwIG\EVkBmgHC{ZYPz[YQhcW5iQ1;TNUBk\WyuczygTWM2OD1yLkigcm0> MlTxNVc6OjR4MU[=
human PBMC MnHMSpVv[3Srb36gZZN{[Xl? MljpNlQhcA>? NVy3OHU2UW6qaXLpeIlwdiCxZjDMVHMucW6mdXPl[EBKVDF{L{KzdFQxKHC{b3T1Z5Rqd25iaX6gbJVu[W5iUFLNR{Bi\nSncjCyOEBpenNiYomgSWxKW0FuIFnDOVA:OSCwTR?= M2TlW|E6OzB7MUW1
HEK293 cells MXfGeY5kfGmxbjDhd5NigQ>? Ml\kNlQhcA>? NGjqbJlC\2:waYP0JIFkfGm4aYT5JIF1KGi3bXHuJHZFWiCrbjDISWszQTNiY3XscJMh[XO|ZYPz[YQh[XNiaX7keYN1cW:wIH;mJJRz[W6|Y4LpdJRqd26jbDD0doFve2GldHn2ZZRqd25iYX\0[ZIhOjRiaILzJIJ6KG2xdYPlJI9{fGWxcH;ueIlvKGy3Y3nm[ZJie2VicnXwc5J1\XJiZ3Xu[UBie3OjeTygSWM2OD1zIH7N NWHT[4JNOTd7MESzO|A>
human HL60 cells M1O0TmZ2dmO2aX;uJIF{e2G7 NYnKSZp{UW6mdXP0bY9vKG:oIHj1cYFvKEiONkCg[Iln\mW{ZX70bYF1cW:wIHHzd4V{e2WmIHHzJINmdGy|IILl[JVkcW6pIH7peJJwKGKudXWgeIV1emG8b3zpeY0tKEWGNUC9NUBvVQ>? Mn\QNlE6ODJ{M{W=
human HeLa cells MojxSpVv[3Srb36gZZN{[Xl? M3y1e|E3KGh? M{\zfHRz[W6|YXP0bZZifGmxbjDv[kBISUx2LX\1d4VlKF[GUjDsbYdidmRiYnnu[Ilv\yCmb33hbY4h\XiycnXzd4VlKGmwIHj1cYFvKEinTHGgZ4VtdHNiYX\0[ZIhOTZiaILzJIJ6KGy3Y3nm[ZJie2VicnXwc5J1\XJiZ3Xu[UBie3OjeTygSWM2OD1zIH7N NWjGZ2FtOjJ7NUe4N|Q>
human T47D cells NFGydYZRem:uaX\ldoF1cW:wIHHzd4F6 NFntVI44OiCq M{\nVGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iVES3SEBk\WyuczDhd5Nme3OnZDDhd{Bl\WO{ZXHz[UBqdiClZXzsJI52dWKncjDh[pRmeiB5MjDodpMh[nliV2PUJIF{e2G7LDDJR|UxRTFwMzDuUS=> MkPsNlQ6ODB|M{m=
human peripheral blood mononuclear cells NYfJV3FIWHKxbHnm[ZJifGmxbjDhd5NigQ>? NEfFOldKdiC4aYTyc{BqdmirYnn0bY9vKG:oIIDofZRwcGWvYXfncJV1cW6rbnnuMYlv\HWlZXSgd5RqdXWuYYTpc44hd2ZiaIXtZY4heGW{aYDo[ZJidCCkbH;v[EBud26xboXjcIVieiClZXzsd{Bxem:uaX\ldoF1cW:wLDDFSFUxRTJwNzDuUS=> NX:zU4JmOTFyMECwNVQ>
human Caco-2 cells M4XSRWZ2dmO2aX;uJIF{e2G7 NUjq[5JKTW[oZXP0JI9vKF[GUjD0doFve2O{aYD0bY9v[WxiYXP0bZZqfHliaX6gbJVu[W5iQ3Hjc{0zKGOnbHzzJIlvKHC{ZYPlcoNmKG:oIEWlJIZmfGGuIHPhcIYhe2W{dX2sJGVEPTB;Mz61NkBvVQ>? MUOxPFA2PDJ|MB?=
human MCF7 cells NEPt[5VHfW6ldHnvckBie3OjeR?= NVO5fIw1SWexbnnzeEBi[3Srdnn0fUBifCC8ZXLyZYZqe2hiZ3HsOE1XTFJiTFLEJIV5eHKnc4Pl[EBqdiCqdX3hckBOS0Z5IHPlcIx{KGK7IHz1Z4ln\XKjc3WgdoVxd3K2ZYKg[4Vv\SCkYYPl[EB1emGwc3HjeIl3[XSrb36gZZN{[XluIFXDOVA:PS53IH7N MWOyNlE5ODh|Nx?=
human THP1 cells NUfEO5ZKTnWwY4Tpc44h[XO|YYm= MUPBZ5RqfmG2aX;uJI9nKF[GUjDpckBpfW2jbjDUTHAyKGOnbHzzJIF{e2W|c3XkJIF{KGmwY4LlZZNmKGmwIHPheIhmdGmlaXTpckBidnSrbXnjdo9jcWGuIIDldJRq\GVibWLORUBmgHC{ZYPzbY9vKGK7IGLUMXBEWixiRVO1NF0yOCCwTR?= M2j2RVE6OzB7MUW1
human HaCaT cells MUTGeY5kfGmxbjDhd5NigQ>? M3LnUVI1KGh? Mn7wWJJidnOjY4TpeoF1cW:wIH;mJHZFWiCrbjDoeY1idiCKYVPhWEBk\WyuczDh[pRmeiB{NDDodpMh[nlibIXjbYZmemG|ZTDy[ZBwenSncjDn[Y5mKGG|c3H5MEBGSzVyPUCuN|IyPSEQvF2= NWflNJZbOjZ|NkewNVk>
human HN12 cells MX;Qdo9tcW[ncnH0bY9vKGG|c3H5 NG[5Z3g4OiCq Mni2RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKTkGyJINmdGy|IHHzd4V{e2WmIHHzJIRm[3KnYYPlJIlvKGOnbHygcpVu[mW{IHHmeIVzKDd{IHjyd{BjgSCZU2SgZZN{[XluIFnDOVA:OC53NUOg{txO NXu4bYhDOjR7MECzN|k>
human HaCaT cells MXvGeY5kfGmxbjDhd5NigQ>? NEPHZ5VKdmirYnn0bY9vKG:oIHPvcI9vgSCob4LtZZRqd25ib3[gbJVu[W5iSHHDZXQh[2WubIO= M{jIdlIzPDB2M{K2
human HCT116 cells MWjGeY5kfGmxbjDhd5NigQ>? NV\WT|JJOjBvNECg{txO M3vvfFI1KGh? M2jXTGFod26rc4SgZYN1cX[rdImgZZQhWkGUIDj1cotvd3ewIH;ybYdqdiliZYjwdoV{e2WmIHnuJIh2dWGwIFjDWFEyPiClZXzsd{Bkdy2neIDy[ZN{cW6pIGLBVmUh[XRiMkCgeI8hPDBidV2gZYZ1\XJiMkSgbJJ{KGK7IHz1Z4ln\XKjc3WgdoVxd3K2ZYKg[4Vv\SCjc4PhfS=> M3LTO|I{Ojd4NES5
mouse C3H10T1/2 cells NHXVcWRHfW6ldHnvckBie3OjeR?= M3nSUlAvPS13IN88US=> NV7W[3prOjRiaB?= NXzIUVNtUW6qaXLpeIlwdiCxZjDI[YRo\WixZzDzbYdv[WyrbnegdIF1cHejeTDpckBud3W|ZTDDN2gyOFRzL{KgZ4VtdHNiYYPz[ZN{\WRiYYOg[I94diC{ZXf1cIF1cW:wIH;mJGdtcTFiYYSgNE42KHSxIEWgeW0h[W[2ZYKgNlQhcHK|IHL5JHJVNVCFUjDhcoFtgXOrcx?= M2LCcVIzOjJ4NkW3
human A498 cells NVO3ZolVTnWwY4Tpc44h[XO|YYm= MUKwMlAyKM7:TR?= NHzGRmw1KGh? NIH2cpNKdmS3Y4Tpc44hd2ZiQ2nQNlQhdVKQQTDlfJBz\XO|aX;uJIlvKGi3bXHuJGE1QThiY3XscJMh[XRiMD6wNUDPxE1iYX\0[ZIhPCCqcoOgZpkhWlRvUFPSJIFv[Wy7c3nz NGLqS3kzOTN7Mkm4Ny=>

... 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
Smiles CC(CCCC(C)(C)O)C1CCC2\C(CCCC12C)=C\C=C/3CC(O)CC(O)C3=C

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03029429 Active not 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