Calcitriol

Catalog No.S1466 Batch:S146603

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Technical Data

Formula

C27H44O3
Molecular Weight 416.64 CAS No. 32222-06-3
Solubility (25°C)* In vitro DMSO 83 mg/mL (199.21 mM)
Ethanol 83 mg/mL (199.21 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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. Solutions are unstable and should be 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]

Protocol (from reference)

Cell Assay:

[6]
  • Cell lines

    CLL cells

  • Concentrations

    100 nM

  • Incubation Time

    24 h

  • Method

    CLL cells were treated with DMSO (vehicle control) or calcitriol (100 nM). Cells were harvested at the indicated time points with mild trypsinization
Animal Study:

[7]
  • Animal Models

    Male Sprague–Dawley rats

  • Dosages

    200 ng/kg

  • Administration

    p.o.

Customer Product Validation

Data independently produced by , , Mireia Vila Gasull University of Porto. 2011;Mireia Vila Gasull

Data from [Data independently produced by , , Mol Cell Endocrinol, 2018, 470:1-13]

Data from [Data independently produced by , , Inflammation, 2017, 40(6):1884-1893]

Selleck's Calcitriol has been cited by 55 publications

VDR regulates mitochondrial function as a protective mechanism against renal tubular cell injury in diabetic rats [ Redox Biol, 2024, 70:103062] PubMed: 38320454
Calcitriol impairs the secretion of IL-4 and IL-13 in Th2 cells via modulating VDR-Gata3-Gfi1 axis [ bioRxiv, 2024, ] PubMed: none
In Vivo and In Vitro Evidence for an Interplay between the Glucocorticoid Receptor and the Vitamin D Receptor Signaling [ Cells, 2023, 12(18)2291] PubMed: 37759513
In Vivo and In Vitro Evidence for an Interplay between the Glucocorticoid Receptor and the Vitamin D Receptor Signaling [ Cells, 2023, 12(18)2291] PubMed: 37759513
Vitamin A- and D-Deficient Diets Disrupt Intestinal Antimicrobial Peptide Defense Involving Wnt and STAT5 Signaling Pathways in Mice [ Nutrients, 2023, 15(2)376] PubMed: 36678247
Brk/PTK6 and Involucrin Expression May Predict Breast Cancer Cell Responses to Vitamin D3 [ Int J Mol Sci, 2023, 24(13)10757] PubMed: 37445934
Brk/PTK6 and Involucrin Expression May Predict Breast Cancer Cell Responses to Vitamin D3 [ Int J Mol Sci, 2023, 24(13)10757] PubMed: 37445934
Piscine Vitamin D Receptors Vdra/Vdrb in the Absence of Vitamin D Are Utilized by Grass Carp Reovirus for Promoting Viral Replication [ Microbiol Spectr, 2023, 11(4):e0128723] PubMed: 37466438
Piscine Vitamin D Receptors Vdra/Vdrb in the Absence of Vitamin D Are Utilized by Grass Carp Reovirus for Promoting Viral Replication [ Microbiol Spectr, 2023, 11(4):e0128723] PubMed: 37466438
Vitamin D3 suppresses the cholesterol homeostasis pathway in patient-derived glioma cell lines [ FEBS Open Bio, 2023, 13(9):1789-1806] PubMed: 37489660

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.