Calcitriol (1,25-Dihydroxyvitamin D3)

Alias: 1,25(OH)2D3; 1,25(OH)2-D3; 1,25(OH)2-VD3;1,25-Dihydroxyvitamin D3; Topitriol; Rocaltrol; Topitriol; Calcijex; RO215535; Silkis; Soltriol; 1α,25-Dihydroxyvitamin D3;1α,25(OH)2D3
Cat No.:V1857 Purity: ≥98%
Calcitriol (RO215535, Topitriol; 1,25(OH)2D3)is the metabolically/hormonally active form of vitamin D and avitamin D receptor(VDR) agonist.
Calcitriol (1,25-Dihydroxyvitamin D3) Chemical Structure CAS No.: 32222-06-3
Product category: VD VDR
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
1mg
2mg
5mg
10mg
25mg
50mg
100mg
Other Sizes

Other Forms of Calcitriol (1,25-Dihydroxyvitamin D3):

  • (1S)-Calcitriol (1α,25-Dihydroxy-3-epi-vitamin-D3)
  • Calcitriol D6
  • Calcitriol-d3 (1,25-Dihydroxyvitamin D3-d3)
  • Calcitriol Derivative
Official Supplier of:
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Top Publications Citing lnvivochem Products
Purity & Quality Control Documentation

Purity: ≥98%

Purity: ≥98%

Product Description

Calcitriol (RO215535, Topitriol; 1,25(OH)2D3) is an agonist of the vitamin D receptor (VDR) and the form of vitamin D that is metabolically and hormonally active. When calcitriol is converted, it produces metabolites that are more powerful and act faster than other vitamin D forms. Calcitriol regulates the differentiation, growth, and function of the cell immune system, which plays a major role in maintaining mineral and skeletal homeostasis. Studies conducted in vitro have revealed that calcitriol can inhibit the production of interleukin-1β (IL-1β) and tumor necrosis factor-α (TNF-α) in human peripheral blood cells (PBMC) stimulated by lipopolysaccharide (LPS) in a dose-dependent manner.

Biological Activity I Assay Protocols (From Reference)
Targets
Human Endogenous Metabolite
ln Vitro
Calcitriol is a potent inhibitor of PHA-induced lymphocyte proliferation, achieving 70% suppression of tritiated thymidine incorporation after 72 hours in culture. In a concentration-dependent manner, calcitriol reduces the production of interleukin-2 (IL-2) by PHA-stimulated peripheral blood mononuclear cells.[1]
Calcitriol increases the intracellular calcium concentration ([Ca2+]i) in less than 5 seconds by causing the endoplasmic reticulum to release calcium and forming inositol 1,4, 5-trisphosphate and diacylglycerol.[2]
Calcitriol can both stimulate and prevent the growth of human prostate adenocarcinoma cells. Type IV collagenases' (MMP-2 and MMP-9) secreted levels are selectively decreased by calcitriol.[3]
Calcitriol increases the antitumor activity of platinum-based drugs and exhibits antiproliferative activity in prostatic adenocarcinoma and squamous cell carcinoma. In PC-3 and murine squamous cell carcinoma cells, calcitriol prior to paclitaxel significantly lowers clonogenic survival compared with either agent alone.[4]
Calcitriol is a potent anti-proliferative agent that targets a broad range of cancerous cell types. Growth factor receptor expression is modulated, apoptosis and differentiation are induced, and G0/G1 arrest is increased in response to calcitriol. Calcitriol inhibits the motility and invasiveness of tumor cells as well as the development of new blood vessels, thereby amplifying the antitumor effects of numerous cytotoxic agents.[5]
ln Vivo
Calcitriol treatment (150 ng/kg per day for 4.5 months) improves relaxations (pD2: 6.30±0.09, Emax: 68.6±3.9% in OVX treated with Calcitriol, n=8). Both kidneys of OVX rats have decreased renal blood flow, which is remedied by calcitriol treatment. Chronic calcitriol administration decreases the increased expression of Thromboxane-prostanoid (TP) receptor and COX-2 in the renal arteries of OVX rats[3]. Treatment with high- and low-dose calcitriol reduces the fructose-fed rats' systolic blood pressure (SBP) by 14±4 and 9±4 mmHg, respectively, on day 56. When compared to other groups, high-dose calcitriol treatment (20 ng/kg per day) significantly raises serum ionized calcium levels (1.44±0.05 mmol/L).
Cell Assay
Calcitriol (100 nM) or DMSO (vehicle control) were used to treat CLL cells. At the designated time intervals, cells were harvested with a light trypsinization.
Animal Protocol
150 ng/kg daily, oral gavage
Adult female Sprague-Dawley rats
References

[1]. J Clin Invest . 1984 Oct;74(4):1451-5.

[2]. J Biol Chem . 1997 May 2;272(18):11902-7.

[3]. Cancer Epidemiol Biomarkers Prev . 1997 Sep;6(9):727-32.

[4]. Clin Cancer Res . 2001 Apr;7(4):1043-51.

[5]. J Steroid Biochem Mol Biol . 2004 May;89-90(1-5):519-26./a >

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C27H44O3
Molecular Weight
416.64
Exact Mass
416.33
Elemental Analysis
C, 77.84; H, 10.65; O, 11.52
CAS #
32222-06-3
Appearance
Solid powder
SMILES
C[C@H](CCCC(C)(C)O)[C@H]1CC[C@@H]\2[C@@]1(CCC/C2=C\C=C/3\C[C@H](C[C@@H](C3=C)O)O)C
InChi Key
GMRQFYUYWCNGIN-NKMMMXOESA-N
InChi Code
InChI=1S/C27H44O3/c1-18(8-6-14-26(3,4)30)23-12-13-24-20(9-7-15-27(23,24)5)10-11-21-16-22(28)17-25(29)19(21)2/h10-11,18,22-25,28-30H,2,6-9,12-17H2,1,3-5H3/b20-10+,21-11-/t18-,22-,23-,24+,25+,27-/m1/s1
Chemical Name
(1R,3S,5Z)-5-[(2E)-2-[(1R,3aS,7aR)-1-[(2R)-6-hydroxy-6-methylheptan-2-yl]-7a-methyl-2,3,3a,5,6,7-hexahydro-1H-inden-4-ylidene]ethylidene]-4-methylidenecyclohexane-1,3-diol
Synonyms
1,25(OH)2D3; 1,25(OH)2-D3; 1,25(OH)2-VD3;1,25-Dihydroxyvitamin D3; Topitriol; Rocaltrol; Topitriol; Calcijex; RO215535; Silkis; Soltriol; 1α,25-Dihydroxyvitamin D3;1α,25(OH)2D3
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: ~83 mg/mL (~199.2 mM)
Water: <1 mg/mL
Ethanol: ~83 mg/mL (~199.2 mM)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.4002 mL 12.0008 mL 24.0015 mL
5 mM 0.4800 mL 2.4002 mL 4.8003 mL
10 mM 0.2400 mL 1.2001 mL 2.4002 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

  • Calculate the Mass of a compound required to prepare a solution of known volume and concentration
  • Calculate the Volume of solution required to dissolve a compound of known mass to a desired concentration
  • Calculate the Concentration of a solution resulting from a known mass of compound in a specific volume
An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
  • Enter 350.26 in the Molecular Weight (MW) box
  • Enter 10 in the Concentration box and choose the correct unit (mM)
  • Enter 5 in the Volume box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
  • Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
  • Enter 25 into the Concentration (End) box and select the correct unit (mM)
  • Enter 25 into the Volume (End) box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:
  • To calculate molar mass of a chemical compound, please enter the chemical/molecular formula and click the “Calculate’ button.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
  • Molecular mass (or 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.
/

Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

  • Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
  • Click the “Calculate” button
  • The answer appears in the Volume (to add to vial) box
In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
+
+
+

Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

Clinical Trial Information
NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05415254 Recruiting Drug: Calcitriol COVID-19
Vitamin D Deficiency
RenJi Hospital June 12, 2022 Not Applicable
NCT03748966 Recruiting Drug: Calcitriol X-linked Hypophosphatemia
Hypophosphatemic Rickets
Massachusetts General Hospital March 28, 2019 Early Phase 1
NCT05902078 Not yet recruiting Drug: Eldecalcitol capsules
Drug: Calcitriol capsules
Low Bone Mineral Density
Postmenopausal Osteoporosis
Shanghai Jiao Tong University
Affiliated Sixth People's
Hospital
June 2023 Phase 4
NCT05298163 Not yet recruiting Drug: Calcitriol capsules
Drug: Placebo
Diabetic Kidney Disease Indonesia University April 2022 Not Applicable
NCT02859896 Active
Recruiting
Drug: Doxercalciferol
(GZ427397)
Drug: Calcitriol
Secondary Hyperparathyroidism
-Chronic Kidney Disease
Sanofi Phase 3 Phase 3
Biological Data
  • Calcitriol


    Calcipotriol inducedERαexpression in ER-negative breast cancer cells.

    Calcitriol

    Calcitriol induced ERαprotein expression.2014 Mar 29;14:230. doi: 10.1186/1471-2407-14-230.

  • Calcitriol


    Immunocytochemical analysis of ERαand VDR in primary and established breast cancer cells.2014 Mar 29;14:230. doi: 10.1186/1471-2407-14-230.

    Calcitriol

    Calcitriol induced a fully active ERα.2014 Mar 29;14:230. doi: 10.1186/1471-2407-14-230.

  • Calcitriol


    Calcitriol inducedERαmRNA expression through the VDR in ERα-negative breast cancer cells.2014 Mar 29;14:230. doi: 10.1186/1471-2407-14-230.

Contact Us