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
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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 MVnDfZRwfG:6aXRCpIF{e2G7 MmPvNVIxKGh? NGiwdYNEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJS1RzMU[gZZN{\XO|ZXSgZZMh\GWlcnXhd4UhcW5iY3XscEBkd3WwdDDh[pRmeiBzMkCgbJJ{NCCLQ{WwQVFmNTB3IN88US=> M4j1dFIzQTJ4ME[4
human HOS cells M{TWTGZ2dmO2aX;uJIF{e2G7 Mnm2NlQhcA>? M2\MN2FkfGm4aYT5JIF1KGi3bXHuJHZFWiCneIDy[ZN{\WRiaX6gbJVu[W5iSF;TJINmdGy|IITyZY5{\mWldHXkJJdqfGhicFfMN{1pV2NuIIDDSG5CNWiYRGKgZY5lKHCqUlytWGsh[XO|ZYPz[YQh[XNiYYPz[ZN{\WRiYYOgeJJidnOlcnnweIlwdmGuIHHjeIl3[XSrb36gcYVie3W{ZXSgNlQhcHK|IIDvd5QhcW6oZXP0bY9vKGK7IHz1Z4ln\XKjc3WgdoVxd3K2ZYKg[4Vv\SCjc4PhfUwhTUN3ME2x[U0xPSEQvF2= M1XOWVIyQDh7M{O0
human HOS/SF cells M4npOWZ2dmO2aX;uJIF{e2G7 MWmyOEBp NV3nOFhzXHKjboPhZ5RqfmG2aX;uJI9nKF[GUj3t[YRq[XSnZDDvd5Rmd2OjbHPpckBxem:vb4TldkBqdiCqdX3hckBJV1NxU1[gZ4VtdHNiYX\0[ZIhOjRiaILzJIJ6KGy3Y3nm[ZJie2VicnXwc5J1\XJiZ3Xu[UBie3OjeTygSWM2OD1{Lk\lMVA2KM7:TR?= NEnyRWozPDlyMEeyPC=>
human PBMC NFzPN2dHfW6ldHnvckBie3OjeR?= Mlz4NlQhcA>? MoToTY5pcWKrdHnvckBw\iCOUGOtbY5lfWOnZDDUUmZidHCqYTDwdo9lfWO2aX;uJIlvKGi3bXHuJHBDVUNiYX\0[ZIhOjRiaILzJIJ6KEWOSWPBMEBKSzV;Mj65[U0xPSEQvF2= M1H5TlE6OzB7MUW1
mouse LM05e cells MlTyVJJwdGmoZYLheIlwdiCjc4PhfS=> MY[3NkBp MmjhRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDtc5V{\SCOTUC1[UBk\WyuczDhd5Nme3OnZDDhd{Bl\WO{ZXHz[UBqdiClZXzsJI52dWKncjDh[pRmeiB5MjDodpMh[nliV2PUJIF{e2G7LDDJR|UxRTOnLUC1JO69VQ>? M1;2elI1QTByM{O5
rat osteosarcoma cells NHfjdpVHfW6ldHnvckBie3OjeR?= NG\QeG5KdmS3Y4Tpc44hd2ZiVlTSMY1m\GmjdHXkJFI1NWi7ZILvfJlt[XOnIITyZY5{[3KrcITpc44hcW5icnH0JI9{fGWxc3HyZ49u[SClZXzsd{BjgSCudXPp[oVz[XOnIILldI9zfGW{IHflcoUh[XO|YYmsJGVFPTB;MD6yJI5O MWOyNVkxOjJ|NR?=
rat ROS 17/2.8 cells MXfGeY5kfGmxbjDhd5NigQ>? Ml3CNVYhcA>? M3T0d2FkfGm4aYT5JIF1KF[GUjDpckBz[XRiUl;TJFE4NzJwODDj[YxteyCjc4Pld5Nm\CCjczD0doFve2O{aYD0bY9v[WxiYXP0bZZifGmxbjDv[kAzPC2qeXTyc5h6dGG|ZTDn[Y5mKHC{b33veIVzKGGodHXyJFE3KGi{czDifUBtfWOrZnXyZZNmKHKncH;yeIVzKGenbnWgZZN{[XluIFXDOVA:OC5{IH7N MYmxPVE3Pzh7Mx?=
COS7 cells NVztSYZ4TnWwY4Tpc44h[XO|YYm= NHXQVWMzPCCq M4TUbGFod26rc4SgZYN1cX[rdImgZZQhcHWvYX6gWmRTKGmwIFPPV|ch[2WubIOgZZN{\XO|ZXSgZZMhcW6mdXP0bY9vKG:oIITyZY5{[3KrcITpc45idCC2cnHud4FkfGm4YYTpc44h[W[2ZYKgNlQhcHK|IHL5JI1wfXOnIH;zeIVweG:wdHnuJIx2[2moZYLhd4UhemWyb4L0[ZIh\2WwZTDhd5NigSxiRVO1NF0xNjVibl2= NHWz[28yPzlyNEO3NC=>
mouse SVEC cells MUXQdo9tcW[ncnH0bY9vKGG|c3H5 Ml34O|IhcA>? Moj3RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDtc5V{\SCVVlXDJINmdGy|IHHzd4V{e2WmIHHzJIRm[3KnYYPlJIlvKGOnbHygcpVu[mW{IHHmeIVzKDd{IHjyd{BjgSCZU2SgZZN{[XluIFnDOVA:OC53MjDuUS=> NFrCbZgzPDlyMEOzPS=>
CV1 cells M3mwSGZ2dmO2aX;uJIF{e2G7 NGDyOZFC[3Srdnn0fUBwdiCqdX3hckBXTFJvbXXkbYF1\WRidILhcpNkemmydHnvckBw\iCxc4Tlc4NidGOrbjDWSHJGKG[3c3XkJJRwKHSqeX3p[Ilv\SCtaX7hd4UheHKxbX;0[ZIw\3Kxd4ToJIhwem2xbnWgdoVxd3K2ZYKg[4Vv\SCrbjDDWlEh[2WubIOsJGVFPTB;MD63JI5O MmDsNVcyPDl6OEC=
COS1 cells NX7mOVhSTnWwY4Tpc44h[XO|YYm= NGHJZphFcXOybHHj[Y1mdnRib3[gNU1idHCqYTygNlUuME:KKWuzTH1FOyCocn;tJIh2dWGwIG\EVkBmgHC{ZYPz[YQhcW5iQ1;TNUBk\WyuczygTWM2OD1yLkigcm0> NWT2UIVIOTd7MkS2NVY>
human PBMC MkLUSpVv[3Srb36gZZN{[Xl? M1fsWFI1KGh? M3nOUmlvcGmkaYTpc44hd2ZiTGDTMYlv\HWlZXSgTWwyOi9{M4C0NEBxem:mdXP0bY9vKGmwIHj1cYFvKFCETVOgZYZ1\XJiMkSgbJJ{KGK7IFXMTXNCNCCLQ{WwQVEhdk1? MlziNVk{ODlzNUW=
HEK293 cells NUXSOmRETnWwY4Tpc44h[XO|YYm= M2DGXVI1KGh? MnrJRYdwdmm|dDDhZ5Rqfmm2eTDheEBpfW2jbjDWSHIhcW5iSFXLNlk{KGOnbHzzJIF{e2W|c3XkJIF{KGmwZIXjeIlwdiCxZjD0doFve2O{aYD0bY9v[WxidILhcpNi[3SrdnH0bY9vKGGodHXyJFI1KGi{czDifUBud3W|ZTDvd5Rmd3CxboTpckBtfWOrZnXyZZNmKHKncH;yeIVzKGenbnWgZZN{[XluIFXDOVA:OSCwTR?= MoGwNVc6ODR|N{C=
human HL60 cells MWDGeY5kfGmxbjDhd5NigQ>? NXPLdGhJUW6mdXP0bY9vKG:oIHj1cYFvKEiONkCg[Iln\mW{ZX70bYF1cW:wIHHzd4V{e2WmIHHzJINmdGy|IILl[JVkcW6pIH7peJJwKGKudXWgeIV1emG8b3zpeY0tKEWGNUC9NUBvVQ>? MmfKNlE6ODJ{M{W=
human HeLa cells NIK4[mxHfW6ldHnvckBie3OjeR?= MkKwNVYhcA>? MkfvWJJidnOjY4TpeoF1cW:wIH;mJGdCVDRvZoXz[YQhXkSUIHzp[4Fv\CCkaX7kbY5oKGSxbXHpckBmgHC{ZYPz[YQhcW5iaIXtZY4hUGWOYTDj[YxteyCjZoTldkAyPiCqcoOgZpkhdHWlaX\ldoF{\SC{ZYDvdpRmeiCpZX7lJIF{e2G7LDDFR|UxRTFibl2= Mn3INlI6PTd6M{S=
human T47D cells MlvQVJJwdGmoZYLheIlwdiCjc4PhfS=> MXG3NkBp MXTBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFR2N1SgZ4VtdHNiYYPz[ZN{\WRiYYOg[IVkemWjc3WgbY4h[2WubDDueY1j\XJiYX\0[ZIhPzJiaILzJIJ6KFeVVDDhd5NigSxiSVO1NF0yNjNibl2= MVOyOFkxODN|OR?=
human peripheral blood mononuclear cells NV7rempzWHKxbHnm[ZJifGmxbjDhd5NigQ>? MYPJckB3cXS{bzDpcohq[mm2aX;uJI9nKHCqeYTvbIVu[WepbIX0bY5qdmmwLXnu[JVk\WRic4TpcZVt[XSrb36gc4YhcHWvYX6gdIVzcXCqZYLhcEBjdG:xZDDtc45wdnWlbHXhdkBk\WyuczDwdo9tcW[ncnH0bY9vNCCHREWwQVIvPyCwTR?= NXzpSWh4OTFyMECwNVQ>
human Caco-2 cells NWrR[4hnTnWwY4Tpc44h[XO|YYm= MkLqSYZn\WO2IH;uJHZFWiC2cnHud4NzcXC2aX;uZYwh[WO2aY\peJkhcW5iaIXtZY4hS2Glbz2yJINmdGy|IHnuJJBz\XOnbnPlJI9nKDVnIH\leIFtKGOjbH[gd4VzfW1uIFXDOVA:Oy53MjDuUS=> MkDoNVgxPTR{M{C=
human MCF7 cells Ml\mSpVv[3Srb36gZZN{[Xl? MXLB[49vcXO2IHHjeIl3cXS7IHH0JJpm[nKjZnnzbEBo[Wx2LW\EVkBNSkRiZYjwdoV{e2WmIHnuJIh2dWGwIF3DSlch[2WubIOgZpkhdHWlaX\ldoF{\SC{ZYDvdpRmeiCpZX7lJIJie2WmIITyZY5{[WO2aY\heIlwdiCjc4PhfUwhTUN3ME21MlUhdk1? M4LmO|IzOThyOEO3
human THP1 cells NVXod2dITnWwY4Tpc44h[XO|YYm= Mk\TRYN1cX[jdHnvckBw\iCYRGKgbY4hcHWvYX6gWGhROSClZXzsd{Bie3Onc4Pl[EBieyCrbnPy[YF{\SCrbjDjZZRp\WyrY3nkbY4h[W62aX3pZ5Jw[mmjbDDw[ZB1cWSnIH3SUmEh\XiycnXzd4lwdiCkeTDSWE1RS1JuIFXDOVA:OTBibl2= NXfi[|lrOTl|MEmxOVU>
human HaCaT cells MmO3SpVv[3Srb36gZZN{[Xl? M1y5ZlI1KGh? M1vCUHRz[W6|YXP0bZZifGmxbjDv[kBXTFJiaX6gbJVu[W5iSHHDZXQh[2WubIOgZYZ1\XJiMkSgbJJ{KGK7IHz1Z4ln\XKjc3WgdoVxd3K2ZYKg[4Vv\SCjc4PhfUwhTUN3ME2wMlMzOTVizszN NH3Ze|MzPjN4N{CxPS=>
human HN12 cells NWXVeVlIWHKxbHnm[ZJifGmxbjDhd5NigQ>? MUK3NkBp M3XTTGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSF6xNkBk\WyuczDhd5Nme3OnZDDhd{Bl\WO{ZXHz[UBqdiClZXzsJI52dWKncjDh[pRmeiB5MjDodpMh[nliV2PUJIF{e2G7LDDJR|UxRTBwNUWzJO69VQ>? M1OzTlI1QTByM{O5
human HaCaT cells NETBXJlHfW6ldHnvckBie3OjeR?= M{LsN2lvcGmkaYTpc44hd2ZiY3;sc456KG[xcn3heIlwdiCxZjDoeY1idiCKYVPhWEBk\Wyucx?= MWOyNlQxPDN{Nh?=
human HCT116 cells MUTGeY5kfGmxbjDhd5NigQ>? M1HFT|IxNTRyIN88US=> M1XEelI1KGh? M1vSUWFod26rc4SgZYN1cX[rdImgZZQhWkGUIDj1cotvd3ewIH;ybYdqdiliZYjwdoV{e2WmIHnuJIh2dWGwIFjDWFEyPiClZXzsd{Bkdy2neIDy[ZN{cW6pIGLBVmUh[XRiMkCgeI8hPDBidV2gZYZ1\XJiMkSgbJJ{KGK7IHz1Z4ln\XKjc3WgdoVxd3K2ZYKg[4Vv\SCjc4PhfS=> NGe3e|kzOzJ5NkS0PS=>
mouse C3H10T1/2 cells M3jocWZ2dmO2aX;uJIF{e2G7 NUD6endZOC53LUWg{txO NXzXeYNzOjRiaB?= MYXJcohq[mm2aX;uJI9nKEinZHflbI9oKHOrZ37hcIlv\yCyYYToe4F6KGmwIH3veZNmKEN|SEGwWFEwOiClZXzsd{Bie3Onc4Pl[EBieyCmb4fuJJJm\3WuYYTpc44hd2ZiR3zpNUBifCByLkWgeI8hPSC3TTDh[pRmeiB{NDDodpMh[nliUmStVGNTKGGwYXz5d4l{ MkO2NlIzOjZ4NUe=
human A498 cells NIL5PYNHfW6ldHnvckBie3OjeR?= NFuzRYoxNjBzIN88US=> NFHSRno1KGh? NFHuV2RKdmS3Y4Tpc44hd2ZiQ2nQNlQhdVKQQTDlfJBz\XO|aX;uJIlvKGi3bXHuJGE1QThiY3XscJMh[XRiMD6wNUDPxE1iYX\0[ZIhPCCqcoOgZpkhWlRvUFPSJIFv[Wy7c3nz NYrCN|Q1OjF|OUK5PFM>

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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
Synonyms RO215535, Topitriol

Bio Calculators

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02962102 Not yet recruiting Critically Ill|Acute Kidney Injury David Leaf|National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK)|Brigham and Womens Hospital February 2017 Phase 2
NCT01561222 Not yet recruiting Chronic Kidney Disease Stage 1|Chronic Kidney Disease Stage 2 Taixing Peoples Hospital July 2015 Phase 4
NCT02410005 Active, not recruiting Diabetic Nephropathies Weill Cornell Medical College in Qatar|Weill Medical College of Cornell University|Hamad Medical Corporation October 2014 Phase 2|Phase 3
NCT02224144 Active, not recruiting End Stage Renal Disease|Kidney Transplantation|Bone Loss|Fractures|Vascular Calcifications Columbia University|Satellite Healthcare August 2014 Phase 2
NCT02061384 Active, not recruiting Male Infertility|Klinefelters Syndrome|Y-chromosome Microdeletions University of Washington August 2014 Phase 2
NCT02186665 Completed Plaque Psoriasis Galderma July 2014 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