Calcitriol (RO215535)

Catalog No.S1466 Synonyms: Topitriol, 1,25-Dihydroxyvitamin D3

For research use only.

Calcitriol (RO215535, Topitriol, 1,25-Dihydroxyvitamin D3) 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. Solutions are best fresh-prepared.

Calcitriol (RO215535) Chemical Structure

CAS No. 32222-06-3

Selleck's Calcitriol (RO215535) has been cited by 39 publications

Purity & Quality Control

Choose Selective Vitamin Inhibitors

Biological Activity

Description Calcitriol (RO215535, Topitriol, 1,25-Dihydroxyvitamin D3) 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. Solutions are best fresh-prepared.
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 MkDFR5l1d3SxeHnjxsBie3OjeR?= NGC2cGMyOjBiaB?= MUDDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDIR3QyOTZiYYPz[ZN{\WRiYYOg[IVkemWjc3WgbY4h[2WubDDjc5VvfCCjZoTldkAyOjBiaILzMEBKSzVyPUHlMVA2KM7:TR?= MUC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjl{NkC2PEc,OjJ7Mk[wOlg9N2F-
HOS M{TRZmZ2dmO2aX;uJIF{e2G7 M4XyNGFkfGm4aYT5JIF1KGi3bXHuJHZFWiCneIDy[ZN{\WRiaX6gbJVu[W5iSF;TJINmdGy|IITyZY5{\mWldHXkJJdqfGhicFfMN{1pV2NuIIDDSG5CNWiYRGKgZY5lKHCqUlytWGsh[XO|ZYPz[YQh[XNiYYPz[ZN{\WRiYYOgeJJidnOlcnnweIlwdmGuIHHjeIl3[XSrb36gcYVie3W{ZXSgNlQhcHK|IIDvd5QhcW6oZXP0bY9vKGK7IHz1Z4ln\XKjc3WgdoVxd3K2ZYKg[4Vv\SCjc4PhfUwhTUN3MDC9JFAvODByMEGg{txONg>? M1;yWVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzOEi5N|M1Lz5{MUi4PVM{PDxxYU6=
SK-MEL-188 Ml2yS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MmH4OFghcHK| MUfHdo94fGhiaX7obYJqfGmxbjDv[kBpfW2jbjDTT{1OTUxvMUi4JINmdGy|IH3lZZN2emWmIHHmeIVzKDR6IHjyd{BjgSCPVGOvVG1UKGG|c3H5MEBKSzVyIE2gNE4xODByMTFOwG0v NYfKUXZFRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkewO|A4PzlpPkK3NFcxPzd7PD;hQi=>
osteosarcoma cells MoLVSpVv[3Srb36gZZN{[Xl? MUTF[oZm[3Rib36gWmRTKHS{YX7zZ5JqeHSrb37hcEBi[3Srdnn0fUBqdiCqdX3hckBwe3Snb4PhdoNwdWFiY3XscJMtKEWFNUCgQUAxNjByMECxNFYh|ryPLh?= NFTXV|Q9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOEC1OFI{OCd-MUiwOVQzOzB:L3G+
HOS/SF M1nSXWZ2dmO2aX;uJIF{e2G7 NInFVW0zPCCqcoO= NGHOXVBVemGwc3HjeIl3[XSrb36gc4YhXkSULX3l[IlifGWmIH;zeIVw[2GuY3nuJJBzd22xdHXyJIlvKGi3bXHuJGhQWy:VRjDj[YxteyCjZoTldkAzPCCqcoOgZpkhdHWlaX\ldoF{\SC{ZYDvdpRmeiCpZX7lJIF{e2G7LDDFR|UxKD1iMD6wNFAxOjZizszNMi=> NFHMfoo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEmwNFczQCd-MkS5NFA4Ojh:L3G+
LM05e NIj2WIRCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= NWGxcpZPPzJiaILz M3qw[WFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgcY92e2ViTF2wOYUh[2WubIOgZZN{\XO|ZXSgZZMh\GWlcnXhd4UhcW5iY3XscEBvfW2kZYKgZYZ1\XJiN{KgbJJ{KGK7IGfTWEBie3OjeTygTWM2OCB;IECuNFAxODNizszNMi=> M2XScFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OUCwN|M6Lz5{NEmwNFM{QTxxYU6=
HEK293 M2rMcmZ2dmO2aX;uJIF{e2G7 NU[yZoxjXHKjboPy[ZBz\XO|aX;uJI9nKF[SMU[teIFo\2WmIG\EVkApfW6tbn;3ckBwemmpaX6pJIV5eHKnc4Pl[EBqdiCKRVuyPVMh[2WubIOgbIFz[m:{aX7nJJBEVVhvR1HMOE1PS2:UIHHu[EBOUDFyMDjVRXMqKFhiNITrMWxWSyC{ZYDvdpRmeiCybHHzcYllKGG|c3Xzd4VlKGG|IHnuZ5Jm[XOnIHnuJG5Ed1JicnXjdpVqfG2nboSgZpkh[mW2YT3nZYxi[3Sxc3nkZZNmKHKncH;yeIVzKGenbnWgZoF{\WRibXHtcYFtcWGwIIT3c{1pgWK{aXSgZZN{[XluIFnDOVAhRSByLkCwNFA2KM7:TT6= M1;kSFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7OUi5PFE4Lz5{OUm4PVgyPzxxYU6=
HEK293 NVvMVJk3TnWwY4Tpc44h[XO|YYm= M{L1eXRz[W6|YXP0bZZifGmxbjDv[kBXWDF4LYTh[4dm\CCYRGKgLJVvc26xd36gc5Jq\2mwKTDlfJBz\XO|ZXSgbY4hUEWNMkmzJINmdGy|IHjhdoJwemmwZzDwR21ZNUeDTEStVnhT[WyyaHGgZY5lKE2KMUCwLHVCWyliWDC0eIsuVFWFIILldI9zfGW{IIDsZZNucWRiYYPz[ZN{\WRiYYOgbY5kemWjc3WgbY4hcW62ZYLhZ5Rqd25id3n0bEBTYFKjbIDoZUBjgSCkZYThMYdidGGldH;zbYRie2VicnXwc5J1\XJiZ3Xu[UBj[XOnZDDtZY1u[WyrYX6geJdwNSxiRVO1NEA:KDBwMECwNFch|ryPLh?= MUC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTl6OUixO{c,Ojl7OEm4NVc9N2F-
HEK293T MoTESpVv[3Srb36gZZN{[Xl? NHTrclFC\2:waYP0JIFkfGm4aYT5JIF1KEeDTESgSG5CNWKrbnTpcoch\G:vYXnuJIZ2e2WmIG\EVkApfW6tbn;3ckBwemmpaX6pJIxq\2GwZDDibY5lcW6pIHTvcYFqdiCneIDy[ZN{\WRiaX6gWWFUNWKuYTDISWshOjl|VDDj[YxteyCjc4Pld5Nm\CCjczDi[ZRiNWyjY4ThcYF{\SC2cnHud4NzcXC2aX;uZYwh[WO2aY\heIlwdiCkeTDGVmVVNWKjc3XkJGdmdmWETFH6[ZIh[XO|YYmsJGlEPTBiPTCwMlAxODB7NUOg{txONg>? M{jOOVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMUS0Olk4Lz5|MEG0OFY6PzxxYU6=
HEK293 MnH5SpVv[3Srb36gZZN{[Xl? MV7B[49vcXO2IHHjeIl3cXS7IHH0JHZFWiBqdX7rco94diCxcnnnbY4qKGW6cILld5Nm\CCrbjDISWszQTNiY3XscJMh[2:2cnHud4Zm[3SnZDD3bZRpKE6Fb2KgZZN{\XO|ZXSgZZMh\GWlcnXhd4UhcW5iTlPvVkBz\WO{dXn0cYVvfCCkeTD0e48ucHmkcnnkJIF{e2G7LDDJR|UxKD1iMD6wNFAyKM7:TT6= MXS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjZzM{SyNEc,OjZ4MUO0NlA9N2F-
HEK293 NHP3OopHfW6ldHnvckBie3OjeR?= NVvsUHBvOTZidH:gNlQhcHK| MVHB[49vcXO2IHHjeIl3cXS7IHH0JHZFWiCrbjDoeY1idiCKRVuyPVMh[2WubIOgZZN{\XO|ZXSgZZMhfHKjboPjdolxfGmxbnHsJIFkfGm4aYT5JIFnfGW{IEG2JJRwKDJ2IHjyd{BjgSCudXPp[oVz[XOnIILldI9zfGW{IHflcoUh[XO|YYmsJGVEPTBiPTCwMlAxODF{IN88UU4> NUnDXZc2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[2NVM1OjBpPkK2OlE{PDJyPD;hQi=>
ROS 17/2.8 MYPGeY5kfGmxbjDhd5NigQ>? NUfSeHNrOTZiaILz NETjcZNC[3Srdnn0fUBifCCYRGKgbY4hemG2IGLPV{AyPy9{LkigZ4VtdHNiYYPz[ZN{\WRiYYOgeJJidnOlcnnweIlwdmGuIHHjeIl3[XSrb36gc4YhOjRvaInkdo95gWyjc3Wg[4Vv\SCycn;tc5RmeiCjZoTldkAyPiCqcoOgZpkhdHWlaX\ldoF{\SC{ZYDvdpRmeiCpZX7lJIF{e2G7LDDFR|UxKD1iMD6wNFAzKM7:TT6= MUW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTF4N{i5N{c,OTlzNke4PVM9N2F-
osteosarcoma cells MkfiSpVv[3Srb36gZZN{[Xl? NHj2WIdC[3Srdnn0fUBifCCYRGKgbY4hemG2IH;zeIVwe2G{Y3;tZUBk\WyuczDhd5Nme3OnZDDhd{AzPC2qeXTyc5h6dGG|ZTD0doFve2O{aYD0bY9vKGK7IILldI9zfGW{IHflcoUh[XO|YYmsJGVEPTBiPTCwMlAxODJizszNMi=> MUm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPzl4MEmyOEc,OTd7NkC5NlQ9N2F-
ROS 17/2.8 M33m[WZ2dmO2aX;uJIF{e2G7 NGDIblgyPiCqcoO= MmP6RYN1cX[rdImgZZQhemG2IILlZ49u[mmwYX70JIZ2dGxibHXu[5RpKF[GUjDlfJBz\XO|ZXSgbY4hemG2IGLPV{AyPy9{LkigZ4VtdHNidILhcpNn\WO2ZXSge4l1cCB{ND3ofYRzd3i7bHHz[UBo\W6nIIDyc41wfGW{IHHzd4V{e2WmIHHzJJRz[W6|Y4LpdJRqd26jbDDhZ5RqfmG2aX;uJIFnfGW{IEG2JIhzeyCkeTDseYNq\mW{YYPlJJJmeG:{dHXyJIdmdmViYYPzZZktKEWFNUCgQUAxNjByMEKg{txONg>? M2XkflxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6N{KyNVMxLz5zOEeyNlE{ODxxYU6=
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ROS 17/2.8 M1[1dWZ2dmO2aX;uJIF{e2G7 NIH3Z2QyPiCqcoO= MkD1RYdwdmm|dDDhZ5Rqfmm2eTDheEBz[XRiVlTSJIlvKFKRUzCxO{8zNjhiY3XscJMhfHKjboPm[YN1\WRid3n0bEBEgXB{NHGxJJJmeG:{dHXyJJBt[XOvaXSgZZN{\XO|ZXSgZZMhcW6lcnXhd4UhcW5iQ4nwNlRiOSC2cnHud4NzcXC2aX;uJIFnfGW{IEG2JIhzeyCkeTDseYNq\mW{YYPlJJJmeG:{dHXyJIdmdmViYYPzZZktKEWFNUCgQUAxNjByMEKg{txONg>? NWHFXZVSRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKwNVg6OThpPkKyNFE5QTF6PD;hQi=>
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osteosarcoma cells MonTSpVv[3Srb36gZZN{[Xl? MYHUdoFve2GldHn2ZZRqd25ib3[gWmRTKGmwIILheEBwe3Snb4PhdoNwdWFiY3XscJMh[XO|ZYPz[YQh[XNiMkStbJllem:6eXzhd4UhfHKjboPjdolxfGmxbnHsJIFkfGm4aYT5JIJ6KGy3Y3nm[ZJie2VicnXwc5J1\XJiZ3Xu[UBie3OjeTygSWQ2OCB;IECuNFAxOiEQvF2u MUS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjZ|MES0OEc,OjZ4M{C0OFQ9N2F-
osteosarcoma cells MVHGeY5kfGmxbjDhd5NigQ>? M{nLVFE3KGi{cx?= NIT0RZVKdmirYnn0bY9vKG:oIG\EVk1qdmS3Y3XkJFI1NWi7ZILvfJlt[XOnIITyZY5{[3KrcITpc44hcW5icnH0JI9{fGWxc3HyZ49u[SClZXzsd{Bi\nSncjCxOkBpenNiYomgcJVkcW[ncnHz[UBz\XCxcoTldkBo\W6nIHHzd4F6NCCHREWwJF0hOC5yMECyJO69VS5? NHX1S2w9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkS5NFAyOCd-MkK0PVAxOTB:L3G+
osteosarcoma cells NIO1fY5HfW6ldHnvckBie3OjeR?= NUTVV|lpSWO2aY\peJkh[XRiVlTSJIlvKHKjdDDvd5Rmd3OjcnPvcYEh[2WubIOgZZN{\XO|ZXSgZZMhcW6mdXP0bY9vKG:oIEK0MYh6\HKxeInsZZNmKHKncH;yeIVzKGenbnWgeJJidnOlcnnweIlwdiCkeTDseYNq\mW{YYPlJJJmeG:{dHXyJIdmdmViYYPzZZktKEWFNUCgQUAxNjByMEOg{txONg>? MYS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQThzOUewNkc,OTl6MUm3NFI9N2F-
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Assay
Methods Test Index PMID
Western blot CyclinD1 ; IRE1α / p-eIF2α / eIF2α / Atf4 / CHOP ; p-PERK / PERK ; FGFR1 / FGFR2 / FGFR3 / FGFR4 ; Wnt10b / Wnt16 28643892 29776409 30149605

Protocol (from reference)

Solubility (25°C)

In vitro

DMSO 83 mg/mL
(199.21 mM)
Water Insoluble
Ethanol '''83 mg/mL

Chemical Information

Molecular Weight 416.64
Formula

C27H44O3

CAS No. 32222-06-3
Storage 3 years -20°C powder
Smiles CC(CCCC(C)(C)O)C1CCC2C1(CCCC2=CC=C3CC(CC(C3=C)O)O)C

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04551170 Recruiting Drug: Theophylline|Drug: Placebo Pseudohypoparathyroidism|Albright Hereditary Osteodystrophy|Pseudohypoparathyroidism Type 1a Vanderbilt University Medical Center July 13 2020 Phase 2
NCT03029429 Recruiting Drug: Theophylline|Drug: Placebos Pseudohypoparathyroidism|Albright Hereditary Osteodystrophy Vanderbilt University Medical Center|Harvard University September 1 2018 Phase 2

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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.

Handling Instructions

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