1. Vitamin D Related/Nuclear Receptor
  2. VD/VDR
  3. Maxacalcitol

Maxacalcitol  (Synonyms: 22-Oxacalcitriol)

製品番号: HY-32339 純度: 99.08%
COA 取扱説明書 Technical Support

Maxacalcitol (22-Oxacalcitriol), a vitamin D3 (HY-15398) analog, is an orally active VDR agonist. Maxacalcitol has a limited calcemic effect. Maxacalcitol has the potential for psoriasis and hyperparathyroidism research.

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Maxacalcitol

Maxacalcitol 構造式

CAS 番号 : 103909-75-7

容量 価格(税別) 在庫状況 数量
1 mg $122 在庫あり
5 mg $440 在庫あり
10 mg $680 在庫あり
25 mg $1350 在庫あり
50 mg $2160 在庫あり
100 mg   お問い合わせ  
200 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

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カスタマーレビュー

Based on 4 publication(s) in Google Scholar

Other Forms of Maxacalcitol:

Top Publications Citing Use of Products
  • 生物活性

  • 純度とドキュメンテーション

  • 参考文献

  • カスタマーレビュー

製品説明

Maxacalcitol (22-Oxacalcitriol), a vitamin D3 (HY-15398) analog, is an orally active VDR agonist. Maxacalcitol has a limited calcemic effect. Maxacalcitol has the potential for psoriasis and hyperparathyroidism research[1][2][3].

Cellular Effect
Cell Line Type Value Description References
Caco-2 EC50
144.5 nM
Compound: 22-oxa-1,25(OH)2D3
Activation of VDR in human Caco2 cells expressing lentiviral VDRE-luciferase vector assessed as VDRE-mediated transcriptional activity measured after 24 hrs by luciferase transcriptional reporter assay
Activation of VDR in human Caco2 cells expressing lentiviral VDRE-luciferase vector assessed as VDRE-mediated transcriptional activity measured after 24 hrs by luciferase transcriptional reporter assay
[PMID: 27070779]
Caco-2 EC50
40.8 nM
Compound: 22-oxa-1,25(OH)2D3
Transactivation of VDR in human Caco2 cells after 24 hrs by luciferase reporter gene assay
Transactivation of VDR in human Caco2 cells after 24 hrs by luciferase reporter gene assay
[PMID: 26367019]
HaCaT EC50
159.7 nM
Compound: 22-oxa-1,25(OH)2D3
Activation of VDR in human HaCaT cells expressing lentiviral VDRE-luciferase vector assessed as VDRE-mediated transcriptional activity measured after 24 hrs by luciferase transcriptional reporter assay
Activation of VDR in human HaCaT cells expressing lentiviral VDRE-luciferase vector assessed as VDRE-mediated transcriptional activity measured after 24 hrs by luciferase transcriptional reporter assay
[PMID: 27070779]
HaCaT EC50
37.9 nM
Compound: 22-oxa-1,25(OH)2D3
Transactivation of VDR in human HaCaT cells after 24 hrs by luciferase reporter gene assay
Transactivation of VDR in human HaCaT cells after 24 hrs by luciferase reporter gene assay
[PMID: 26367019]
Jurkat EC50
0.855 nM
Compound: 22-oxa-1,25(OH)2D3
Activation of VDR in human Jurkat cells expressing lentiviral VDRE-luciferase vector assessed as VDRE-mediated transcriptional activity measured after 24 hrs by luciferase transcriptional reporter assay
Activation of VDR in human Jurkat cells expressing lentiviral VDRE-luciferase vector assessed as VDRE-mediated transcriptional activity measured after 24 hrs by luciferase transcriptional reporter assay
[PMID: 27070779]
Keratinocyte IC50
22.6 nM
Compound: 2, maxacalcitol
Antiproliferative activity against human keratinocyte assessed as inhibition of [3H]TdR uptake
Antiproliferative activity against human keratinocyte assessed as inhibition of [3H]TdR uptake
[PMID: 16630723]
体外実験

Maxacalcitol (22-Oxacalcitriol; 100 nM; for 24 h) markedly increases the expression of LL-37 mRNA in Ca9-22 cells and modestly but significantly increases in HSC-2, HSC-3, and HSC-4 cells[1].

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

RT-PCR[1]

Cell Line: Human gingival/oral epithelial cells
Concentration: 100 nM
Incubation Time: 24 h
Result: Markedly increased the expression of LL-37 mRNA 77-fold in human gingival epithelial Ca9-22 cells and modestly but significantly increased in human oral epithelial HSC-2, HSC-3, and HSC-4 cells.
体内実験

Maxacalcitol (22-Oxacalcitriol; oral gavage; 15 µg/kg/day; 14 days) followed by GSK 269962 at a single dose of 10 mg/kg, leads to a statistically significant reduction of intercontraction interval and bladder compliance, and an increase in DO index, without any effect on ANVC, FNVC, and VTNVC[2].
Maxacalcitol in a dose of 30 but not 15 µg/kg/day induced reduction in detrusor overactivity (DO) index, non-voiding contractions frequency (FNVC), and amplitude (ANVC), while increasing volume threshold to elicit non-voiding contractions (VTNVC)[2].

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

Animal Model: Female Wistar rats (weighting 200-225 g)[2]
Dosage: 15 µg/kg
Administration: Oral gavage; daily; 14 days
Result: Followed by GSK 269962 at a single dose of 10 mg/kg, led to a statistically significant reduction of intercontraction interval and bladder compliance, and an increase in DO index, without any effect on ANVC, FNVC, and VTNVC.
臨床実験
分子量

418.61

分子式

C26H42O4

CAS 番号
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](OCCC(C)(O)C)C)CCC/2)[H])O)O

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

4°C, protect from light, stored under nitrogen

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

溶剤 & 溶解度
体外: 

DMSO : 50 mg/mL (119.44 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 2.3889 mL 11.9443 mL 23.8886 mL
5 mM 0.4778 mL 2.3889 mL 4.7777 mL
10 mM 0.2389 mL 1.1944 mL 2.3889 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
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Concentration
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Volume
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Molecular Weight *

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

一般には略語で表示されます:C1V1 = C2V2

濃度 (開始)

C1

×
体積 (開始)

V1

=
濃度 (終了)

C2

×
体積 (終了)

V2

体内:

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: ≥ 1.67 mg/mL (3.99 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 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% (20% SBE-β-CD in Saline)

    Solubility: ≥ 1.67 mg/mL (3.99 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

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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.
純度とドキュメンテーション

純度: 99.71%

参考文献

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 2.3889 mL 11.9443 mL 23.8886 mL 59.7215 mL
5 mM 0.4778 mL 2.3889 mL 4.7777 mL 11.9443 mL
10 mM 0.2389 mL 1.1944 mL 2.3889 mL 5.9721 mL
15 mM 0.1593 mL 0.7963 mL 1.5926 mL 3.9814 mL
20 mM 0.1194 mL 0.5972 mL 1.1944 mL 2.9861 mL
25 mM 0.0956 mL 0.4778 mL 0.9555 mL 2.3889 mL
30 mM 0.0796 mL 0.3981 mL 0.7963 mL 1.9907 mL
40 mM 0.0597 mL 0.2986 mL 0.5972 mL 1.4930 mL
50 mM 0.0478 mL 0.2389 mL 0.4778 mL 1.1944 mL
60 mM 0.0398 mL 0.1991 mL 0.3981 mL 0.9954 mL
80 mM 0.0299 mL 0.1493 mL 0.2986 mL 0.7465 mL
100 mM 0.0239 mL 0.1194 mL 0.2389 mL 0.5972 mL
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  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

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

一般には略語で表示されます:C1V1 = C2V2

濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
× = ×
C1   V1   C2   V2
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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製品名:
Maxacalcitol
製品番号:
HY-32339
数量:
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