2. Vitamin D Related/Nuclear Receptor
  3. VD/VDR
  4. Doxercalciferol

Doxercalciferol  (Synonyms: 1.alpha.-Hydroxyvitamin D2)

Cat. No.: HY-32348 Purity: 99.92%
SDS COA Handling Instructions

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Doxercalciferol is a Vitamin D2 analog, acts as an activator of Vitamin D receptor, and prevent renal disease.

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

Doxercalciferol Chemical Structure

Doxercalciferol Chemical Structure

CAS No. : 54573-75-0

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Based on 5 publication(s) in Google Scholar

Other Forms of Doxercalciferol:

Doxercalciferol Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

Doxercalciferol is a Vitamin D2 analog, acts as an activator of Vitamin D receptor, and prevent renal disease.

IC50 & Target

Vitamin D receptor[1]
In Vivo

Doxercalciferol (0.083, 0.167 or 0.333 μg/kg, i.p.) elevates serum phosphorus at Week 6 in 5/6 nephrectomized (NX) rats. Doxercalciferol (0.167 and 0.333 μg/kg) also increases serum calcium and Ca × P at Weeks 2 and 6, and enhances increased pulse wave velocity (PWV) at Week 6 in 5/6 nephrectomized (NX) rats. Doxercalciferol blocks PTH from rising at 0.083 μg/kg, and lowers serum PTH to the SHAM level[1]. Doxercalciferol (125 ng/kg, i.p. thrice per week) increases expression of VDR mRNA level and renal expression of TRPV5 in NON mice fed a HF diet. Doxercalciferol also improves proteinuria, prevents loss of podocytes, and accumulation of extracellular matrix proteins in HF diet-induced mice. Doxercalciferol inhibits the expression of profibrotic growth factors (TGF-β, PAI-1, and connective tissue growth factor (CTGF)), and blocks increased expression of the renin-angiotensin-aldosterone system in mice fed a HF diet. Furthermore, Doxercalciferol suppresses macrophage infiltration, decreases NF-κb activity, and preventes expression of proinflammatory cytokine and the increase in renal lipid accumulation in mice fed a HF diet[2]. Doxercalciferol (30 ng/kg, i.p. thrice per week) prevents albuminuria, markedly attenuates podocyte loss and apoptosis, and reduces glomerular fibrosis in streptozotocin-induced diabetic mice[3].

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

412.65

Formula

C28H44O2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

C=C1[C@H](C[C@@H](C/C1=C/C=C2[C@]3([C@@](C)([C@H](CC3)[C@@H](/C=C/[C@@H](C(C)C)C)C)CCC/2)[H])O)O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, protect from light

*The compound is unstable in solutions, freshly prepared is recommended.

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (242.34 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4234 mL 12.1168 mL 24.2336 mL
5 mM 0.4847 mL 2.4234 mL 4.8467 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

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

    Solubility: ≥ 2.5 mg/mL (6.06 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (6.06 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*The compound is unstable in solutions, freshly prepared is recommended.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.92%

SDS (479 KB)

COA (252 KB) HNMR (141 KB) RP-HPLC (90 KB)

Handling Instructions (2659 KB)
References
Animal Administration
[1]

Rats[1]
Male, Sprague-Dawley, 5/6 nephrectomized (NX) rats (∼200 gm) are used 1 week after nephrectomy. The nephrectomy is performed using a standard two-step surgical ablation procedure. Beginning 2 weeks post-nephrectomy, rats are maintained on a high phosphorus diet (0.9% phosphorus and 0.6% calcium) for the duration of the study to induce secondary hyperparathyroidism. On Day 0, SHAM and 5/6 NX rats (n = 7-10 per group) receive vehicle (5% EtOH/95% propylene glycol; 0.4 mL/kg; i.p.) or VDRA (paricalcitol or Doxercalciferol; 0.083, 0.167 or 0.333 μg/kg; intraperitoneally) three times per week for 41 days (n = 6-10 per group). These doses are chosen based on the fact that lower doses (0.021 and 0.042 μg/kg; i.p.) of either compound are not PTH suppressive after 2 or 6 weeks of treatment in this model of CKD. On Days 0, 13 and 41, blood is collected (24 h post-dose). On Days 0, 13 and 41 (24 h post-dose), animals are anaesthetized with ketamine (50 mg/kg) and blood is collected via the tail vein for PTH and serum blood chemistry determinations[1].

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

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.4234 mL 12.1168 mL 24.2336 mL 60.5840 mL
5 mM 0.4847 mL 2.4234 mL 4.8467 mL 12.1168 mL
10 mM 0.2423 mL 1.2117 mL 2.4234 mL 6.0584 mL
15 mM 0.1616 mL 0.8078 mL 1.6156 mL 4.0389 mL
20 mM 0.1212 mL 0.6058 mL 1.2117 mL 3.0292 mL
25 mM 0.0969 mL 0.4847 mL 0.9693 mL 2.4234 mL
30 mM 0.0808 mL 0.4039 mL 0.8078 mL 2.0195 mL
40 mM 0.0606 mL 0.3029 mL 0.6058 mL 1.5146 mL
50 mM 0.0485 mL 0.2423 mL 0.4847 mL 1.2117 mL
60 mM 0.0404 mL 0.2019 mL 0.4039 mL 1.0097 mL
80 mM 0.0303 mL 0.1515 mL 0.3029 mL 0.7573 mL
100 mM 0.0242 mL 0.1212 mL 0.2423 mL 0.6058 mL
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Doxercalciferol Related Classifications

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.

Keywords:

Doxercalciferol54573-75-01.alpha.-Hydroxyvitamin D2VD/VDRVitamin DVitamin D receptorInhibitorinhibitorinhibit

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