2. PROTAC Metabolic Enzyme/Protease
  3. Molecular Glues Phosphatase
  4. Voclosporin

Voclosporin  (Synonyms: ISAtx-247)

製品番号: HY-106638 純度: 99.85%
COA 取扱説明書

Molarity Calculator

Voclosporin (ISAtx-247) is a calcineurin (PP2B) (CN) inhibitor.

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Voclosporin 構造式

Voclosporin 構造式

CAS 番号 : 515814-01-4

容量 価格（税別） 在庫状況 数量
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 962 在庫あり
Solution
10 mM * 1 mL in DMSO USD 962 在庫あり
Solid
1 mg USD 170 在庫あり
5 mg USD 450 在庫あり
10 mg USD 720 在庫あり
25 mg USD 1440 在庫あり
50 mg USD 2300 在庫あり
100 mg USD 3680 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

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Based on 1 publication(s) in Google Scholar

Voclosporin 関連抗体

Top Publications Citing Use of Products

  • 生物活性

  • プロトコル

  • 純度とドキュメンテーション

  • 参考文献

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製品説明

Voclosporin (ISAtx-247) is a calcineurin (PP2B) (CN) inhibitor[1].

IC50 & Target

Calcineurin[1]
体外実験

This novel semi-synthetic calcineurin (CN) inhibitor is designated Voclosporin (ISATX247). The efficacy of Voclosporin as an immunosuppressive agent is examined using an in vitro calcineurin assay[1]. Voclosporin (ISATX247) is a calcineurin inhibitor that has shown more potency than Cyclosporine in vitro[2].

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

Voclosporin 関連抗体
体内実験

All animals tolerate Voclosporin (ISATX247) and Cyclosporine A (CsA) very well. There are no severe adverse effects associated with either drug. In the Voclosporin group, all animals except 1 have diarrhea of different durations during the study (mean 2.3 days, range 2 to 7 days). This differs from the CsA and the control groups, where no animals have diarrhea. Mean weight loss at the end of the study is slightly higher in the Voclosporin group than in the CsA and control groups (3.4% vs 2.0% and 1.0%, respectively)[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
臨床実験
分子量

1214.62

分子式

C63H111N11O12
CAS 番号
Appearance

Solid

Color

White to off-white

SMILES

C=C/C=C/C[C@@H](C)[C@H]([C@]1([H])N(C([C@](N(C([C@@H](N(C([C@](N(C([C@H](NC([C@@H](NC([C@H](CC(C)C)N(C)C([C@@](C(C)C)([H])NC([C@H](CC(C)C)N(C)C(CN(C)C([C@H](CC)NC1=O)=O)=O)=O)=O)=O)C)=O)C)=O)C)([H])CC(C)C)=O)C)CC(C)C)=O)C)([H])C(C)C)=O)C)O
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

DMSO : ≥ 50 mg/mL (41.17 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.8233 mL 4.1165 mL 8.2330 mL
5 mM 0.1647 mL 0.8233 mL 1.6466 mL
10 mM 0.0823 mL 0.4117 mL 0.8233 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • 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

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    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (2.06 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 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: 99.85%

COA (246 KB) HNMR (429 KB) RP-HPLC (256 KB) LCMS (90 KB)

取扱説明書 (2659 KB)
参考文献
動物実験
[2]

Monkey[2]
Wild-caught, male cynomolgus monkeys, weighing between 5 and 8 kg, are used. Four groups of animals are treated twice daily at 8:00 AM and 6:00 PM for 7 days with the following doses: Group I (n=6), Voclosporin 25 mg/kg; Group II (n=6), Voclosporin 50 mg/kg; Group III (n=5), CsA 25 mg/kg; and Group IV (n=4), vehicle (no drug) 1 mL/kg. Levels of Cyclosporine and Voclosporin in whole blood are measured by liquid chromatography/mass spectrometry[2].

MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
参考文献

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 0.8233 mL 4.1165 mL 8.2330 mL 20.5826 mL
5 mM 0.1647 mL 0.8233 mL 1.6466 mL 4.1165 mL
10 mM 0.0823 mL 0.4117 mL 0.8233 mL 2.0583 mL
15 mM 0.0549 mL 0.2744 mL 0.5489 mL 1.3722 mL
20 mM 0.0412 mL 0.2058 mL 0.4117 mL 1.0291 mL
25 mM 0.0329 mL 0.1647 mL 0.3293 mL 0.8233 mL
30 mM 0.0274 mL 0.1372 mL 0.2744 mL 0.6861 mL
40 mM 0.0206 mL 0.1029 mL 0.2058 mL 0.5146 mL
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Voclosporin Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

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

Keywords:

Voclosporin515814-01-4ISAtx-247ISAtx247ISAtx 247Molecular GluesPhosphataseInhibitorinhibitorinhibit

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製品名:
Voclosporin
製品番号:
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