2. Vitamin D Related/Nuclear Receptor
    Metabolic Enzyme/Protease
  3. VD/VDR
    Endogenous Metabolite
  4. Calcitriol

Calcitriol  (Synonyms: 1,25-Dihydroxyvitamin D3)

Cat. No.: HY-10002 Purity: 99.81%
COA Handling Instructions

Calcitriol is the most active metabolite of vitamin D and also a vitamin D receptor (VDR) agonist.

For research use only. We do not sell to patients.

Calcitriol Chemical Structure

Calcitriol Chemical Structure

CAS No. : 32222-06-3

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Customer Review

Based on 30 publication(s) in Google Scholar

Other Forms of Calcitriol:

Top Publications Citing Use of Products

    Calcitriol purchased from MCE. Usage Cited in: Int Immunopharmacol. 2017 Jun;47:182-189.  [Abstract]

    The total number of sneezing and nasal rubbing motions is significantly reduced by 1,25-(OH)2D3, n=9.

    Calcitriol purchased from MCE. Usage Cited in: Oncotarget. 2017 Oct 26;8(59):100187-100195.  [Abstract]

    Calcitriol increases the expressions of JMJD3 and p16INK4A. 786-O cells are treated with vehicle (Veh) or 100nM Calcitriol (Cal) for 48h, and untreated group as control (Con). The expressions of JMJD3 and p16INK4A are determined with western blotting.

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Calcitriol is the most active metabolite of vitamin D and also a vitamin D receptor (VDR) agonist.

    IC50 & Target

    Human Endogenous Metabolite

     

    In Vitro

    Calcitriol exerts antiproliferative effects on cervical cancer cells in vitro. Cells decrease by 12.8% when treated with 100 nM Calcitriol for 6 days, compare with control. Inhibition of cell proliferation becomes more pronounced with the increase in Calcitriol concentration. The decrease is 26.1% and 31.6% for 200 and 500 nM Calcitriol, respectively. Treatment with Calcitriol for 72 h induces an evident accumulation of cells in the G1 phase, with approximately 66.18% in 200 nM and 78.10% in 500 nM, compare with the control (24.36%). Calcitriol treatment significantly decreases HCCR-1 protein expression compare with the control in a time- and dose-dependent manner[1]. Calcitriol significantly increases ERα mRNA in a dose dependent manner with an EC50 of 9.8×10-9 M[2].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    In Vivo

    Chronic treatment with Calcitriol (150 ng/kg per day for 4.5 months) improves the relaxations (pD2: 6.30±0.09, Emax: 68.6±3.9% in Calcitriol-treated OVX, n=8). Renal blood flow in OVX rats is reduced in both kidneys, and the flow is restored by Calcitriol treatment. The increased expression of COX-2 and Thromboxane-prostanoid (TP) receptor in OVX rat renal arteries is reduced by chronic calcitriol administration[3]. High- and low-dose Calcitriol treatment significantly decreases the systolic blood pressure (SBP) in the fructose-fed rats by 14±4 and 9±4 mmHg, respectively, at Day 56. High-dose Calcitriol treatment (20 ng/kg per day) significantly increases serum ionized calcium level (1.44±0.05 mmol/L) compare with the other groups[4].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Clinical Trial
    Molecular Weight

    416.64

    Appearance

    Solid

    Formula

    C27H44O3
    CAS No.
    SMILES

    C=C1[[email protected]](C[[email protected]@H](C/C1=C/C=C2[[email protected]]3([[email protected]@](C)([[email protected]](CC3)[[email protected]@H](CCCC(C)(O)C)C)CCC/2)[H])O)O
    Structure Classification
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    -20°C, protect from light, stored under nitrogen

    *The compound is unstable in solutions, freshly prepared is recommended.
    Solvent & Solubility
    In Vitro: 

    DMSO : 110 mg/mL (264.02 mM; Need ultrasonic)

    Ethanol : 100 mg/mL (240.02 mM; Need ultrasonic)

    H2O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 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
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: 2.75 mg/mL (6.60 mM); Suspended solution; Need ultrasonic

    • 2.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 2.75 mg/mL (6.60 mM); Clear solution

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.75 mg/mL (6.60 mM); Clear solution

    • 4.

      Add each solvent one by one:  5% DMSO    40% PEG300    5% Tween-80    50% saline

      Solubility: ≥ 2.75 mg/mL (6.60 mM); Clear solution

    • 5.

      Add each solvent one by one:  5% DMSO    95% (20% SBE-β-CD in saline)

      Solubility: ≥ 2.75 mg/mL (6.60 mM); Clear solution

    • 6.

      Add each solvent one by one:  10% EtOH    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.5 mg/mL (6.00 mM); Clear solution

    • 7.

      Add each solvent one by one:  10% EtOH    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 2.5 mg/mL (6.00 mM); Clear solution

    • 8.

      Add each solvent one by one:  10% EtOH    90% corn oil

      Solubility: ≥ 2.5 mg/mL (6.00 mM); Clear solution

    • 9.

      Add each solvent one by one:  1% DMSO    99% saline

      Solubility: 0.55 mg/mL (1.32 mM); Suspended solution; Need ultrasonic

    *All of the co-solvents are available by MCE.
    Purity & Documentation

    Purity: 99.81%

    COA (252 KB) HNMR (184 KB) RP-HPLC (264 KB)

    Handling Instructions (2659 KB)
    References
    Cell Assay
    [1]

    HeLa S3 cells are plated at a density of 1,000 cells/well in 96-well plates of Dulbecco’s modified Eagle’s medium (DMEM) with 10% fetal bovine serum (FBS), treated with 1% ethanol (control) or various concentrations of Calcitriol (100, 200, and 500 nM) for 72 h. A Cell Counting Kit8 (CCK-8) is used to determine cell proliferation. At 24, 48, 72, 96, 120, and 144 h after culturing with 200 nM Calcitriol, cells are harvested for analysis. Three independent experiments are performed in quadruplicate[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [3]

    Adult female Sprague-Dawley rats weighing 200 to 220g are used in this study. Rats are housed in a temperature-controlled room (~23°C) with a 12-h light/dark cycle. The animals have free access to a standard diet and water. Ovariectomy (OVX) is performed on rats. At 6 months after the surgical procedure, the OVX rats are randomly assigned to either treatment with vehicle dimethyl sulfoxide (OVX+vehicle) or Calcitriol (150 ng/kg daily, OVX+calcitriol). Calcitriol treatment is given by oral gavage and lasted or 4.5 months. Blood pressure and serum Calcitriol level are measured[3].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    References
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    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

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    × = ×
    C1   V1   C2   V2

    Keywords:

    Calcitriol32222-06-31,25-Dihydroxyvitamin D3VD/VDREndogenous MetaboliteVitamin DVitamin D receptorInhibitorinhibitorinhibit

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