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Calcitriol

For research use only.

Catalog No.S1466 Synonyms: RO215535, Topitriol

27 publications

Calcitriol Chemical Structure

CAS No. 32222-06-3

Calcitriol (RO215535, Topitriol) 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 27 publications

Purity & Quality Control

Choose Selective Vitamin Inhibitors

Biological Activity

Description Calcitriol (RO215535, Topitriol) 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 MnnPR5l1d3SxeHnjxsBie3OjeR?= MVexNlAhcA>? M1OxNmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGhEXDFzNjDhd5Nme3OnZDDhd{Bl\WO{ZXHz[UBqdiClZXzsJINwfW62IHHmeIVzKDF{MDDodpMtKEmFNUC9NYUuODVizszN NFrNZWs9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkmyOlA3QCd-MkK5NlYxPjh:L3G+
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C3H10T1/2 M1LkbGZ2dmO2aX;uJIF{e2G7 NUnFSVF{OC53IIXN MV:yOEBpenN? NI\ZcVFKdmirYnn0bY9vKG:oIHjl[IdmcG:pIIPp[45idGmwZzDwZZRpf2G7IHnuJI5wdi22YYLn[ZRqdmdic3nSUmEhfHKnYYTl[EBud3W|ZTDDN2gyOFRzL{KgZ4VtdHNiYYPz[ZN{\WRiYYOg[YZn\WO2IH;uJHZFWiCneIDy[ZN{cW:wIHH0JFAvPSC3TTDh[pRmeiB{NDDodpMh[nlicWDDVkBidmGueYPpdy=> NIHkZlg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEezNFk5PCd-MkS3N|A6QDR:L3G+
C3H10T1/2 MVTGeY5kfGmxbjDhd5NigQ>? MV:wMlUhfU1? M{i3ZlI1KGi{cx?= M4nlZWlvcGmkaYTpc44hd2ZiaHXk[4Vpd2dic3nncoFtcW6pIIDheIh4[XliaX6gWmRTNWuwb3Pr[I94diCvb4Xz[UBEO0hzMGSxM|Ih[2WubIOgZZN{\XO|ZXSgZZMh\W[oZXP0JI9vKF[GUjDlfJBz\XO|aX;uJIF1KDBwNTD1UUBi\nSncjCyOEBpenNiYomgdXBEWiCjbnHsfZNqew>? MmjZQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR5M{C5PFQoRjJ2N{OwPVg1RC:jPh?=
LX2 NWLOWJJlTnWwY4Tpc44h[XO|YYm= NI[yfHgyODBibl2= M4LyWFI1KGi{cx?= NWXQdFBlXHKjboPhZ5RqfmG2aX;uJI9nKF[GUjDpckBpfW2jbjDMXFIh[2WubIOgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDUS2Zj\XSjMT3pcoR2[2WmIFPPUFFCOSCvUl7BJIV5eHKnc4Ppc44h[XRiMUCwJI5OKGGodHXyJFI1KGi{czDifUBSNVCFUjDhcoFtgXOrcx?= MWC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODN3MEm5PUc,OzB|NUC5PVk9N2F-
ROS 17/2.8 NWHSWmF{TnWwY4Tpc44h[XO|YYm= M4fiSVE3KGi{cx?= M3XDbmlv\HWldHnvckBw\iCYRGKgeJJidnOlcnnweIlwdmGuIHHjeIl3cXS7IHHzd4V{e2WmIHHzJIFkfGm4YYTpc44hd2ZiMkStbJllem:6eXzhd4Uh\2WwZTDlfJBz\XO|aX;uJIlvKHKjdDDSU3MhOTdxMj64JINmdGy|IHHmeIVzKDF4IHjyd{BjgSCudXPp[oVz[XOnIILldJJ1\XJiYYPzZZk> MVy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjV5NEmyNUc,OjZ3N{S5NlE9N2F-
HL60 NYf2ZZNoTnWwY4Tpc44h[XO|YYm= M3jJWlMxKHSxIEGwNFAhdk1? M{T2PVQ5KGi{cx?= NXjGcmg6UW6mdXP0bY9vKG:oIHPlcIwh\GmoZnXy[Y51cWG2aX;uJIlvKGi3bXHuJGhNPjBiY3XscJMh[XO|ZYPz[YQh[XNibXH0eZJqdmdibX;ydIhwdG:paXPhcEBkcGGwZ3XzJIF1KDNyIITvJFExODBibl2gZYZ1\XJiNEigbJJ{KGK7IGfybYdpfCe|LVfp[Y1{[SC|dHHpcolv\y2kYYPl[EBnd3K2eTDtbYNzd3Olb4DpZ{B3cWW5IHHzd4F6 MV28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTF{N{G0PUc,OjVzMkexOFk9N2F-
SW480-ADH MWDGeY5kfGmxbjDhd5NigQ>? MV6xNFAhdk1? MoXFOFghcHK| MlPxTY5lfWO2aX;uJI9nKGi3bXHuJHNYPDhyLVHETEBk\WyuIHTp[oZmemWwdHnheIlwdiCjc4Pld5Nm\CCjczDmc5Ju[XSrb36gc4Yh[2:vcHHjeEBmeGm2aHXsbY9q\CCrc3zhcoR{KG:oIHjp[4htgSCjZHjldoVvfCClZXzsd{BifCBzMDCnMVchVSCjZoTldkA1QCCqcoOgZpkheGijc3WtZ49vfHKjc4SgcYlkem:|Y3;wfS=> NWHaUY5GRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK5PFk{PzlpPkKyPVg6Ozd7PD;hQi=>
SW480-ADH NH3ScWdHfW6ldHnvckBie3OjeR?= NV3NbZhHOTBibl2= NGqyfHo1QCCqcoO= NFfMSnJKdmS3Y4Tpc44hd2ZiaIXtZY4hW1d2OECtRWRJKGOnbHyg[Iln\mW{ZX70bYF1cW:wIHHzd4V{e2WmIHHzJIZwem2jdHnvckBw\iClb33wZYN1KGWyaYTo[Yxqd2mmIHnzcIFv\HNib3[gbIlocGy7IHHkbIVz\W62IHPlcIx{KGG2IEGwJEcuQCCPIHHmeIVzKDR6IHjyd{BjgSCyaHHz[U1kd262cnHzeEBucWO{b4Pjc5B6 NHvXb2I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Mkm4PVM4QSd-MkK5PFk{Pzl:L3G+
MCF7 M1H2NWFvfGmycn;sbYZmemG2aY\lJIF{e2G7 M2mwSFExOCCwTR?= MVG0PEBpenN? M4\UPGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVPGO{Bk\WyuczDheEAyOCBpLUegUUBi\nSncjC0PEBpenNiYomgUXRVKGG|c3H5JJJmdGG2aY\lJJRwKHWwdILlZZRm\C2lb370do9t M{TnclxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{OUi5N|c6Lz5{Mkm4PVM4QTxxYU6=
CLL M1n2OGZ2dmO2aX;uJIF{e2G7 NH\OUJUyODBibl2= NXHQ[3RUOjRiaILz NVrqdWtDTW[oZXP0JI9vKEO\UEK0RVEhcW5iaIXtZY4heHKrbXHyfUBEVExiY3XscJMh[XO|ZYPz[YQh[XNiaX7jdoVie2ViaX6gWmRTNXKnZ4XsZZRm\CCJQVTEOFVidHCqYTDtVm5CKGW6cILld5Nqd25iYYSgNVAxKG6PIHnuZ5Vj[XSnZDDmc5IhOjRiaILzJIJ6KHG3YX70bZRifGm4ZTDSWE1RS1JibXX0bI9l NXrmW5dLRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWxOFg{QTJpPkK1NVQ5Ozl{PD;hQi=>
CLL NGjDOnpHfW6ldHnvckBie3OjeR?= MUGxNFAhdk1? Mo\XNlQhcHK| NH:0PXdG\m[nY4Sgc44hS1mSMkTBNUBqdiCqdX3hckBxemmvYYL5JGNNVCClZXzsd{Bie3Onc4Pl[EBieyCrbnPy[YF{\SCrbjDWSHIuemWpdXzheIVlKEOGS16xRUBuWk6DIHX4dJJme3Orb36gZZQhOTByIH7NJIlv[3WkYYTl[EBnd3JiMkSgbJJ{KGK7IIH1ZY51cXSjdHn2[UBTXC2SQ2KgcYV1cG:m M3XhTlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MUS4N|kzLz5{NUG0PFM6OjxxYU6=

... 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)C1CCC2C1(CCCC2=CC=C3CC(CC(C3=C)O)O)C

In vivo Formulation Calculator (Clear solution)

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Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

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* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

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Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

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
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

Tech Support

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Handling Instructions

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID