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

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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 MmLkR5l1d3SxeHnjxsBie3OjeR?= Mnj6NVIxKGh? NW\oUI14S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUEOWMUG2JIF{e2W|c3XkJIF{KGSnY4LlZZNmKGmwIHPlcIwh[2:3boSgZYZ1\XJiMUKwJIhzeyxiSVO1NF0y\S1yNTFOwG0> NWq5PYhPOjJ7Mk[wOlg>
human HOS cells NHfq[m1HfW6ldHnvckBie3OjeR?= MWWyOEBp NYLVcFFHSWO2aY\peJkh[XRiaIXtZY4hXkSUIHX4dJJme3OnZDDpckBpfW2jbjDIU3Mh[2WubIOgeJJidnOoZXP0[YQhf2m2aDDwS2w{NWiRYzygdGNFVkFvaG\EVkBidmRicHjSUE1VUyCjc4Pld5Nm\CCjczDhd5Nme3OnZDDhd{B1emGwc3PybZB1cW:wYXygZYN1cX[jdHnvckBu\WG|dYLl[EAzPCCqcoOgdI9{fCCrbn\lZ5Rqd25iYomgcJVkcW[ncnHz[UBz\XCxcoTldkBo\W6nIHHzd4F6NCCHQ{WwQVFmNTB3IN88US=> M4e4elIyQDh7M{O0
human HOS/SF cells M4XTVWZ2dmO2aX;uJIF{e2G7 MWiyOEBp MlzSWJJidnOjY4TpeoF1cW:wIH;mJHZFWi2vZXTpZZRm\CCxc4Tlc4NidGOrbjDwdo9ud3SncjDpckBpfW2jbjDIU3MwW0ZiY3XscJMh[W[2ZYKgNlQhcHK|IHL5JIx2[2moZYLhd4UhemWyb4L0[ZIh\2WwZTDhd5NigSxiRVO1NF0zNj[nLUC1JO69VQ>? MVGyOFkxODd{OB?=
human PBMC NH;U[YxHfW6ldHnvckBie3OjeR?= Mn7vNlQhcA>? MUPJcohq[mm2aX;uJI9nKEySUz3pcoR2[2WmIGTOSoFteGijIIDyc4R2[3Srb36gbY4hcHWvYX6gVGJOSyCjZoTldkAzPCCqcoOgZpkhTUyLU1GsJGlEPT1{LknlMVA2KM7:TR?= NUnhO2h6OTl|MEmxOVU>
mouse LM05e cells MYnQdo9tcW[ncnH0bY9vKGG|c3H5 M4e3NFczKGh? M2fYUmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgcY92e2ViTF2wOYUh[2WubIOgZZN{\XO|ZXSgZZMh\GWlcnXhd4UhcW5iY3XscEBvfW2kZYKgZYZ1\XJiN{KgbJJ{KGK7IGfTWEBie3OjeTygTWM2OD1|ZT2wOUDPxE1? M13OTVI1QTByM{O5
rat osteosarcoma cells NH;qOnNHfW6ldHnvckBie3OjeR?= MWLJcoR2[3Srb36gc4YhXkSULX3l[IlifGWmIEK0MYh6\HKxeInsZZNmKHS{YX7zZ5JqeHSrb36gbY4hemG2IH;zeIVwe2G{Y3;tZUBk\WyuczDifUBtfWOrZnXyZZNmKHKncH;yeIVzKGenbnWgZZN{[XluIFXEOVA:OC5{IH7N NGDMUWozOTlyMkKzOS=>
rat ROS 17/2.8 cells M2LXXWZ2dmO2aX;uJIF{e2G7 MWSxOkBp MXzBZ5Rqfmm2eTDheEBXTFJiaX6gdoF1KFKRUzCxO{8zNjhiY3XscJMh[XO|ZYPz[YQh[XNidILhcpNkemmydHnvcoFtKGGldHn2ZZRqd25ib3[gNlQucHmmcn;4fYxie2ViZ3Xu[UBxem:vb4TldkBi\nSncjCxOkBpenNiYomgcJVkcW[ncnHz[UBz\XCxcoTldkBo\W6nIHHzd4F6NCCHQ{WwQVAvOiCwTR?= MXmxPVE3Pzh7Mx?=
COS7 cells M3nre2Z2dmO2aX;uJIF{e2G7 M2XsUFI1KGh? NVjrc3pOSWexbnnzeEBi[3Srdnn0fUBifCCqdX3hckBXTFJiaX6gR29UPyClZXzsd{Bie3Onc4Pl[EBieyCrbnT1Z5Rqd25ib3[geJJidnOlcnnweIlwdmGuIITyZY5{[WO2aY\heIlwdiCjZoTldkAzPCCqcoOgZpkhdW:3c3Wgc5N1\W:yb370bY4hdHWlaX\ldoF{\SC{ZYDvdpRmeiCpZX7lJIF{e2G7LDDFR|UxRTBwNTDuUS=> MmjsNVc6ODR|N{C=
mouse SVEC cells MXjQdo9tcW[ncnH0bY9vKGG|c3H5 NGL4RWE4OiCq MVrBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IH3veZNmKFOYRVOgZ4VtdHNiYYPz[ZN{\WRiYYOg[IVkemWjc3WgbY4h[2WubDDueY1j\XJiYX\0[ZIhPzJiaILzJIJ6KFeVVDDhd5NigSxiSVO1NF0xNjV{IH7N NFrXUGozPDlyMEOzPS=>
CV1 cells MmCySpVv[3Srb36gZZN{[Xl? MlfMRYN1cX[rdImgc44hcHWvYX6gWmRTNW2nZHnheIVlKHS{YX7zZ5JqeHSrb36gc4Yhd3O2ZX;jZYxkcW5iVlTSSUBnfXOnZDD0c{B1cHmvaXTpcoUhc2mwYYPlJJBzd22xdHXyM4dzd3e2aDDoc5Jud26nIILldI9zfGW{IHflcoUhcW5iQ2[xJINmdGy|LDDFSFUxRTBwNzDuUS=> M3TPZlE4OTR7OEiw
COS1 cells NVTMZXBlTnWwY4Tpc44h[XO|YYm= MWnEbZNxdGGlZX3lcpQhd2ZiMT3hcJBp[SxiMkWtLG9JMVt|SG3EN{Bnem:vIHj1cYFvKF[GUjDlfJBz\XO|ZXSgbY4hS0:VMTDj[YxteyxiSVO1NF0xNjhibl2= M4S2bVE4QTJ2NkG2
human PBMC MXzGeY5kfGmxbjDhd5NigQ>? MkLlNlQhcA>? MmH4TY5pcWKrdHnvckBw\iCOUGOtbY5lfWOnZDDJUFEzNzJ|cESwJJBzd2S3Y4Tpc44hcW5iaIXtZY4hWEKPQzDh[pRmeiB{NDDodpMh[nliRVzJV2EtKEmFNUC9NUBvVQ>? MlTxNVk{ODlzNUW=
HEK293 cells MkfuSpVv[3Srb36gZZN{[Xl? M4f0flI1KGh? MYrB[49vcXO2IHHjeIl3cXS7IHH0JIh2dWGwIG\EVkBqdiCKRVuyPVMh[2WubIOgZZN{\XO|ZXSgZZMhcW6mdXP0bY9vKG:oIITyZY5{[3KrcITpc45idCC2cnHud4FkfGm4YYTpc44h[W[2ZYKgNlQhcHK|IHL5JI1wfXOnIH;zeIVweG:wdHnuJIx2[2moZYLhd4UhemWyb4L0[ZIh\2WwZTDhd5NigSxiRVO1NF0yKG6P M4DGelE4QTB2M{ew
human HL60 cells MlPxSpVv[3Srb36gZZN{[Xl? MmflTY5lfWO2aX;uJI9nKGi3bXHuJGhNPjBiZHnm[oVz\W62aXH0bY9vKGG|c3Xzd4VlKGG|IHPlcIx{KHKnZIXjbY5oKG6rdILvJIJtfWVidHX0doF7d2yrdX2sJGVFPTB;MTDuUS=> MVGyNVkxOjJ|NR?=
human HeLa cells MXrGeY5kfGmxbjDhd5NigQ>? NHfaSnUyPiCq NI[ycG9VemGwc3HjeIl3[XSrb36gc4YhT0GOND3meZNm\CCYRGKgcIlo[W6mIHLpcoRqdmdiZH;tZYlvKGW6cILld5Nm\CCrbjDoeY1idiCKZVzhJINmdGy|IHHmeIVzKDF4IHjyd{BjgSCudXPp[oVz[XOnIILldI9zfGW{IHflcoUh[XO|YYmsJGVEPTB;MTDuUS=> NFHTbWQzOjl3N{izOC=>
human T47D cells NF3oW41Rem:uaX\ldoF1cW:wIHHzd4F6 MljjO|IhcA>? Mk\2RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCWNEfEJINmdGy|IHHzd4V{e2WmIHHzJIRm[3KnYYPlJIlvKGOnbHygcpVu[mW{IHHmeIVzKDd{IHjyd{BjgSCZU2SgZZN{[XluIFnDOVA:OS5|IH7N NXPIXGRxOjR7MECzN|k>
human peripheral blood mononuclear cells NXnI[FhwWHKxbHnm[ZJifGmxbjDhd5NigQ>? NE\sTlFKdiC4aYTyc{BqdmirYnn0bY9vKG:oIIDofZRwcGWvYXfncJV1cW6rbnnuMYlv\HWlZXSgd5RqdXWuYYTpc44hd2ZiaIXtZY4heGW{aYDo[ZJidCCkbH;v[EBud26xboXjcIVieiClZXzsd{Bxem:uaX\ldoF1cW:wLDDFSFUxRTJwNzDuUS=> M3TMeVEyODByMEG0
human Caco-2 cells NFvQZmhHfW6ldHnvckBie3OjeR?= M1nMXGVn\mWldDDvckBXTFJidILhcpNkemmydHnvcoFtKGGldHn2bZR6KGmwIHj1cYFvKEOjY3:tNkBk\WyuczDpckBxemW|ZX7j[UBw\iB3JTDm[ZRidCClYXzmJJNmenWvLDDFR|UxRTNwNUKgcm0> MYmxPFA2PDJ|MB?=
human MCF7 cells MkewSpVv[3Srb36gZZN{[Xl? MU\B[49vcXO2IHHjeIl3cXS7IHH0JJpm[nKjZnnzbEBo[Wx2LW\EVkBNSkRiZYjwdoV{e2WmIHnuJIh2dWGwIF3DSlch[2WubIOgZpkhdHWlaX\ldoF{\SC{ZYDvdpRmeiCpZX7lJIJie2WmIITyZY5{[WO2aY\heIlwdiCjc4PhfUwhTUN3ME21MlUhdk1? MoC0NlIyQDB6M{e=
human THP1 cells NYixW5hHTnWwY4Tpc44h[XO|YYm= M4TYN2FkfGm4YYTpc44hd2ZiVlTSJIlvKGi3bXHuJHRJWDFiY3XscJMh[XO|ZYPz[YQh[XNiaX7jdoVie2ViaX6gZ4F1cGWuaXPp[IlvKGGwdHntbYNzd2KrYXygdIVxfGmmZTDtVm5CKGW6cILld5Nqd25iYomgVnQuWEOULDDFR|UxRTFyIH7N MVexPVMxQTF3NR?=
human HaCaT cells M2LxU2Z2dmO2aX;uJIF{e2G7 MYKyOEBp MlvXWJJidnOjY4TpeoF1cW:wIH;mJHZFWiCrbjDoeY1idiCKYVPhWEBk\WyuczDh[pRmeiB{NDDodpMh[nlibIXjbYZmemG|ZTDy[ZBwenSncjDn[Y5mKGG|c3H5MEBGSzVyPUCuN|IyPSEQvF2= M3vHcVI3OzZ5MEG5
human HN12 cells NWTlbWVxWHKxbHnm[ZJifGmxbjDhd5NigQ>? M3LHO|czKGh? Mm\XRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKTkGyJINmdGy|IHHzd4V{e2WmIHHzJIRm[3KnYYPlJIlvKGOnbHygcpVu[mW{IHHmeIVzKDd{IHjyd{BjgSCZU2SgZZN{[XluIFnDOVA:OC53NUOg{txO MXuyOFkxODN|OR?=
human HaCaT cells MnPoSpVv[3Srb36gZZN{[Xl? NEfGcnBKdmirYnn0bY9vKG:oIHPvcI9vgSCob4LtZZRqd25ib3[gbJVu[W5iSHHDZXQh[2WubIO= M1jhc|IzPDB2M{K2
human HCT116 cells NV\yVVRKTnWwY4Tpc44h[XO|YYm= MWeyNE01OCEQvF2= M{OwO|I1KGh? NUPYPIIzSWexbnnzeEBi[3Srdnn0fUBifCCUQWKgLJVvc26xd36gc5Jq\2mwKTDlfJBz\XO|ZXSgbY4hcHWvYX6gTGNVOTF4IHPlcIx{KGOxLXX4dJJme3OrbnegVmFTTSCjdDCyNEB1dyB2MDD1UUBi\nSncjCyOEBpenNiYomgcJVkcW[ncnHz[UBz\XCxcoTldkBo\W6nIHHzd4F6 MkjpNlMzPzZ2NEm=
mouse C3H10T1/2 cells MV;GeY5kfGmxbjDhd5NigQ>? NVi1OHU5OC53LUWg{txO MX[yOEBp MYHJcohq[mm2aX;uJI9nKEinZHflbI9oKHOrZ37hcIlv\yCyYYToe4F6KGmwIH3veZNmKEN|SEGwWFEwOiClZXzsd{Bie3Onc4Pl[EBieyCmb4fuJJJm\3WuYYTpc44hd2ZiR3zpNUBifCByLkWgeI8hPSC3TTDh[pRmeiB{NDDodpMh[nliUmStVGNTKGGwYXz5d4l{ MkO4NlIzOjZ4NUe=
human A498 cells Mn3qSpVv[3Srb36gZZN{[Xl? NUnISYg6OC5yMTFOwG0> NXX5VoxGPCCq NIq1OoJKdmS3Y4Tpc44hd2ZiQ2nQNlQhdVKQQTDlfJBz\XO|aX;uJIlvKGi3bXHuJGE1QThiY3XscJMh[XRiMD6wNUDPxE1iYX\0[ZIhPCCqcoOgZpkhWlRvUFPSJIFv[Wy7c3nz Mk\6NlE{QTJ7OEO=

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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

Bio Calculators

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03261336 Terminated Castration-resistant Prostate Cancer Donald Trump MD|Inova Health Care Services January 6 2017 Phase 2
NCT03140449 Completed Facial Angiofibroma National Taiwan University Hospital September 5 2013 Phase 3
NCT02125279 Active not recruiting Psoriasis Vulgaris Galderma May 2014 Phase 4
NCT01863641 Unknown status Systemic Lupus Erythematosus Guilan University of Medical Sciences April 2013 Phase 2
NCT01820832 Unknown status Chronic Kidney Disease|Proteinuria Huashan Hospital March 2013 Phase 4
NCT01766440 Completed Plaque Psoriasis Galderma March 2013 Phase 4

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID