Calcitriol

For research use only.

Catalog No.S1466 Synonyms: RO215535, Topitriol

16 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 16 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 NXjIfoNTS3m2b4TvfIlkyqCjc4PhfS=> NW\EXZVpOTJyIHi= MnToR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTGNVOTF4IHHzd4V{e2WmIHHzJIRm[3KnYYPlJIlvKGOnbHygZ492dnRiYX\0[ZIhOTJyIHjyd{whUUN3ME2x[U0xPSEQvF2= NYLXN|A2OjJ7Mk[wOlg>
human HOS cells NU\iPYprTnWwY4Tpc44h[XO|YYm= MojrNlQhcA>? NWD6UIpRSWO2aY\peJkh[XRiaIXtZY4hXkSUIHX4dJJme3OnZDDpckBpfW2jbjDIU3Mh[2WubIOgeJJidnOoZXP0[YQhf2m2aDDwS2w{NWiRYzygdGNFVkFvaG\EVkBidmRicHjSUE1VUyCjc4Pld5Nm\CCjczDhd5Nme3OnZDDhd{B1emGwc3PybZB1cW:wYXygZYN1cX[jdHnvckBu\WG|dYLl[EAzPCCqcoOgdI9{fCCrbn\lZ5Rqd25iYomgcJVkcW[ncnHz[UBz\XCxcoTldkBo\W6nIHHzd4F6NCCHQ{WwQVFmNTB3IN88US=> M4Llc|IyQDh7M{O0
human HOS/SF cells NFjuXItHfW6ldHnvckBie3OjeR?= Mn;sNlQhcA>? M3;LSXRz[W6|YXP0bZZifGmxbjDv[kBXTFJvbXXkbYF1\WRib4P0[Y9k[WylaX6gdJJwdW:2ZYKgbY4hcHWvYX6gTG9UN1OIIHPlcIx{KGGodHXyJFI1KGi{czDifUBtfWOrZnXyZZNmKHKncH;yeIVzKGenbnWgZZN{[XluIFXDOVA:Oi54ZT2wOUDPxE1? MWCyOFkxODd{OB?=
human PBMC M2DheGZ2dmO2aX;uJIF{e2G7 NGXYZ2MzPCCq NFH3Z3pKdmirYnn0bY9vKG:oIFzQV{1qdmS3Y3XkJHRPTmGucHjhJJBzd2S3Y4Tpc44hcW5iaIXtZY4hWEKPQzDh[pRmeiB{NDDodpMh[nliRVzJV2EtKEmFNU2yMllmNTB3IN88US=> MVOxPVMxQTF3NR?=
mouse LM05e cells M2K5XnBzd2yrZnXyZZRqd25iYYPzZZk> NUjoTIVrPzJiaB?= NH\kUnRCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JI1wfXOnIFzNNFVmKGOnbHzzJIF{e2W|c3XkJIF{KGSnY4LlZZNmKGmwIHPlcIwhdnWvYnXyJIFnfGW{IEeyJIhzeyCkeTDXV3Qh[XO|YYmsJGlEPTB;M3WtNFUh|ryP MVWyOFkxODN|OR?=
rat osteosarcoma cells NWq4[Y5uTnWwY4Tpc44h[XO|YYm= M4rD[Wlv\HWldHnvckBw\iCYRGKtcYVlcWG2ZXSgNlQucHmmcn;4fYxie2VidILhcpNkemmydHnvckBqdiC{YYSgc5N1\W:|YYLjc41iKGOnbHzzJIJ6KGy3Y3nm[ZJie2VicnXwc5J1\XJiZ3Xu[UBie3OjeTygSWQ2OD1yLkKgcm0> MUSyNVkxOjJ|NR?=
rat ROS 17/2.8 cells MWjGeY5kfGmxbjDhd5NigQ>? M1;SfFE3KGh? M2D2dWFkfGm4aYT5JIF1KF[GUjDpckBz[XRiUl;TJFE4NzJwODDj[YxteyCjc4Pld5Nm\CCjczD0doFve2O{aYD0bY9v[WxiYXP0bZZifGmxbjDv[kAzPC2qeXTyc5h6dGG|ZTDn[Y5mKHC{b33veIVzKGGodHXyJFE3KGi{czDifUBtfWOrZnXyZZNmKHKncH;yeIVzKGenbnWgZZN{[XluIFXDOVA:OC5{IH7N MUexPVE3Pzh7Mx?=
COS7 cells MX3GeY5kfGmxbjDhd5NigQ>? NH6xXZQzPCCq Mn6yRYdwdmm|dDDhZ5Rqfmm2eTDheEBpfW2jbjDWSHIhcW5iQ1;TO{Bk\WyuczDhd5Nme3OnZDDhd{BqdmS3Y4Tpc44hd2ZidILhcpNkemmydHnvcoFtKHS{YX7zZYN1cX[jdHnvckBi\nSncjCyOEBpenNiYomgcY92e2Vib4P0[Y9xd262aX6gcJVkcW[ncnHz[UBz\XCxcoTldkBo\W6nIHHzd4F6NCCHQ{WwQVAvPSCwTR?= NEHIXo0yPzlyNEO3NC=>
mouse SVEC cells MUnQdo9tcW[ncnH0bY9vKGG|c3H5 MkXTO|IhcA>? MX;BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IH3veZNmKFOYRVOgZ4VtdHNiYYPz[ZN{\WRiYYOg[IVkemWjc3WgbY4h[2WubDDueY1j\XJiYX\0[ZIhPzJiaILzJIJ6KFeVVDDhd5NigSxiSVO1NF0xNjV{IH7N MnXhNlQ6ODB|M{m=
CV1 cells MUPGeY5kfGmxbjDhd5NigQ>? NGi5eWRC[3Srdnn0fUBwdiCqdX3hckBXTFJvbXXkbYF1\WRidILhcpNkemmydHnvckBw\iCxc4Tlc4NidGOrbjDWSHJGKG[3c3XkJJRwKHSqeX3p[Ilv\SCtaX7hd4UheHKxbX;0[ZIw\3Kxd4ToJIhwem2xbnWgdoVxd3K2ZYKg[4Vv\SCrbjDDWlEh[2WubIOsJGVFPTB;MD63JI5O MYKxO|E1QTh6MB?=
COS1 cells MXXGeY5kfGmxbjDhd5NigQ>? M2TvTGRqe3CuYXPlcYVvfCCxZjCxMYFteGijLDCyOU0pV0hrW{PIYWQ{KG[{b32gbJVu[W5iVlTSJIV5eHKnc4Pl[EBqdiCFT2OxJINmdGy|LDDJR|UxRTBwODDuUS=> MlTlNVc6OjR4MU[=
human PBMC M3vBdWZ2dmO2aX;uJIF{e2G7 NEK1OXIzPCCq NYO4ZYNCUW6qaXLpeIlwdiCxZjDMVHMucW6mdXPl[EBKVDF{L{KzdFQxKHC{b3T1Z5Rqd25iaX6gbJVu[W5iUFLNR{Bi\nSncjCyOEBpenNiYomgSWxKW0FuIFnDOVA:OSCwTR?= NV\yenNTOTl|MEmxOVU>
HEK293 cells NGO0e5hHfW6ldHnvckBie3OjeR?= NEHoPGgzPCCq NVvzWGJESWexbnnzeEBi[3Srdnn0fUBifCCqdX3hckBXTFJiaX6gTGVMOjl|IHPlcIx{KGG|c3Xzd4VlKGG|IHnu[JVkfGmxbjDv[kB1emGwc3PybZB1cW:wYXygeJJidnOjY4TpeoF1cW:wIHHmeIVzKDJ2IHjyd{BjgSCvb4Xz[UBwe3Snb4DvcpRqdiCudXPp[oVz[XOnIILldI9zfGW{IHflcoUh[XO|YYmsJGVEPTB;MTDuUS=> M4G2R|E4QTB2M{ew
human HL60 cells MXrGeY5kfGmxbjDhd5NigQ>? M2PMW2lv\HWldHnvckBw\iCqdX3hckBJVDZyIHTp[oZmemWwdHnheIlwdiCjc4Pld5Nm\CCjczDj[YxteyC{ZXT1Z4lv\yCwaYTyc{BjdHWnIITleJJigm:uaYXtMEBGTDVyPUGgcm0> NYPzSlczOjF7MEKyN|U>
human HeLa cells MWnGeY5kfGmxbjDhd5NigQ>? NWDEeXBHOTZiaB?= MYTUdoFve2GldHn2ZZRqd25ib3[gS2FNPC2odYPl[EBXTFJibHnnZY5lKGKrbnTpcoch\G:vYXnuJIV5eHKnc4Pl[EBqdiCqdX3hckBJ\UyjIHPlcIx{KGGodHXyJFE3KGi{czDifUBtfWOrZnXyZZNmKHKncH;yeIVzKGenbnWgZZN{[XluIFXDOVA:OSCwTR?= NYf1RWQxOjJ7NUe4N|Q>
human T47D cells NHv4eYlRem:uaX\ldoF1cW:wIHHzd4F6 NIG5O|k4OiCq M1jiPGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iVES3SEBk\WyuczDhd5Nme3OnZDDhd{Bl\WO{ZXHz[UBqdiClZXzsJI52dWKncjDh[pRmeiB5MjDodpMh[nliV2PUJIF{e2G7LDDJR|UxRTFwMzDuUS=> MYiyOFkxODN|OR?=
human peripheral blood mononuclear cells NXXaXFJZWHKxbHnm[ZJifGmxbjDhd5NigQ>? NUTuZ5RTUW5idnn0do8hcW6qaXLpeIlwdiCxZjDwbJl1d2inbXHn[4x2fGmwaX7pck1qdmS3Y3XkJJN1cW23bHH0bY9vKG:oIHj1cYFvKHCncnnwbIVz[WxiYnzvc4QhdW:wb371Z4xm[XJiY3XscJMheHKxbHnm[ZJifGmxbjygSWQ2OD1{Lkegcm0> NF;vUoYyOTByMECxOC=>
human Caco-2 cells Mor1SpVv[3Srb36gZZN{[Xl? M2LCfGVn\mWldDDvckBXTFJidILhcpNkemmydHnvcoFtKGGldHn2bZR6KGmwIHj1cYFvKEOjY3:tNkBk\WyuczDpckBxemW|ZX7j[UBw\iB3JTDm[ZRidCClYXzmJJNmenWvLDDFR|UxRTNwNUKgcm0> MkixNVgxPTR{M{C=
human MCF7 cells NH7VN3dHfW6ldHnvckBie3OjeR?= NUXsSnhVSWexbnnzeEBi[3Srdnn0fUBifCC8ZXLyZYZqe2hiZ3HsOE1XTFJiTFLEJIV5eHKnc4Pl[EBqdiCqdX3hckBOS0Z5IHPlcIx{KGK7IHz1Z4ln\XKjc3WgdoVxd3K2ZYKg[4Vv\SCkYYPl[EB1emGwc3HjeIl3[XSrb36gZZN{[XluIFXDOVA:PS53IH7N MWeyNlE5ODh|Nx?=
human THP1 cells M4nCR2Z2dmO2aX;uJIF{e2G7 MkTQRYN1cX[jdHnvckBw\iCYRGKgbY4hcHWvYX6gWGhROSClZXzsd{Bie3Onc4Pl[EBieyCrbnPy[YF{\SCrbjDjZZRp\WyrY3nkbY4h[W62aX3pZ5Jw[mmjbDDw[ZB1cWSnIH3SUmEh\XiycnXzd4lwdiCkeTDSWE1RS1JuIFXDOVA:OTBibl2= Mm\iNVk{ODlzNUW=
human HaCaT cells NGfZXY1HfW6ldHnvckBie3OjeR?= MV6yOEBp NUWxVpFyXHKjboPhZ5RqfmG2aX;uJI9nKF[GUjDpckBpfW2jbjDIZWNiXCClZXzsd{Bi\nSncjCyOEBpenNiYomgcJVkcW[ncnHz[UBz\XCxcoTldkBo\W6nIHHzd4F6NCCHQ{WwQVAvOzJzNTFOwG0> MXmyOlM3PzBzOR?=
human HN12 cells M1fCSnBzd2yrZnXyZZRqd25iYYPzZZk> MlLSO|IhcA>? MnjURY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKTkGyJINmdGy|IHHzd4V{e2WmIHHzJIRm[3KnYYPlJIlvKGOnbHygcpVu[mW{IHHmeIVzKDd{IHjyd{BjgSCZU2SgZZN{[XluIFnDOVA:OC53NUOg{txO NEHwTmUzPDlyMEOzPS=>
human HaCaT cells MV;GeY5kfGmxbjDhd5NigQ>? NFLaOHJKdmirYnn0bY9vKG:oIHPvcI9vgSCob4LtZZRqd25ib3[gbJVu[W5iSHHDZXQh[2WubIO= MUKyNlQxPDN{Nh?=
human HCT116 cells MmDOSpVv[3Srb36gZZN{[Xl? M2XFRVIxNTRyIN88US=> MYmyOEBp M17YSmFod26rc4SgZYN1cX[rdImgZZQhWkGUIDj1cotvd3ewIH;ybYdqdiliZYjwdoV{e2WmIHnuJIh2dWGwIFjDWFEyPiClZXzsd{Bkdy2neIDy[ZN{cW6pIGLBVmUh[XRiMkCgeI8hPDBidV2gZYZ1\XJiMkSgbJJ{KGK7IHz1Z4ln\XKjc3WgdoVxd3K2ZYKg[4Vv\SCjc4PhfS=> NVjEO5Q4OjN{N{[0OFk>
mouse C3H10T1/2 cells M3WxbWZ2dmO2aX;uJIF{e2G7 M1rUd|AvPS13IN88US=> M1HNR|I1KGh? MkWyTY5pcWKrdHnvckBw\iCKZXTn[Yhw\yC|aXfuZYxqdmdicHH0bJdigSCrbjDtc5V{\SCFM1ixNHQyNzJiY3XscJMh[XO|ZYPz[YQh[XNiZH;3ckBz\We3bHH0bY9vKG:oIFfsbVEh[XRiMD61JJRwKDVidV2gZYZ1\XJiMkSgbJJ{KGK7IGLUMXBEWiCjbnHsfZNqew>? MW[yNlIzPjZ3Nx?=
human A498 cells M4frZmZ2dmO2aX;uJIF{e2G7 M2\UdVAvODFizszN M2HscVQhcA>? M3vOVmlv\HWldHnvckBw\iCFWWCyOEBuWk6DIHX4dJJme3Orb36gbY4hcHWvYX6gRVQ6QCClZXzsd{BifCByLkCxJO69VSCjZoTldkA1KGi{czDifUBTXC2SQ2KgZY5idHm|aYO= M1nSVVIyOzl{OUiz

... 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