1. Metabolic Enzyme/Protease Cell Cycle/DNA Damage Epigenetics
  2. Oxidative Phosphorylation HDAC
  3. TYA-018

TYA-018 is an orally active, potent and highly selective HDAC6 inhibitor. TYA-018 can protect heart function in mice. TYA-018 also enhances energetics in mice by increasing expression of targets associated with fatty acid metabolism, protein metabolism, and oxidative phosphorylation.

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TYA-018

TYA-018 構造式

CAS 番号 : 2653254-31-8

容量 価格(税別) 在庫状況 数量
>無料サンプル (0.1 - 0.2 mg)   今すぐ申し込む  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 275 在庫あり
Solution
10 mM * 1 mL in DMSO USD 275 在庫あり
Solid
5 mg $250 在庫あり
10 mg $410 在庫あり
25 mg $820 在庫あり
50 mg $1300 在庫あり
100 mg $2100 在庫あり
200 mg   お問い合わせ  
500 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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製品説明

TYA-018 is an orally active, potent and highly selective HDAC6 inhibitor. TYA-018 can protect heart function in mice. TYA-018 also enhances energetics in mice by increasing expression of targets associated with fatty acid metabolism, protein metabolism, and oxidative phosphorylation[1].

IC50 & Target

HDAC6

 

体内実験

TYA-018 (15 mg/kg, Oral gavage, daily, for 8 weeks) protects against sarcomere damage and reduced Nppb expression in BAG3cKO mice[1].

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

Animal Model: BAG3cKO mice[1]
Dosage: 15 mg/kg
Administration: Oral gavage, daily, starting at 2 months old, for 8 weeks
Result: Conferred cardioprotection in mice. Significantly reduced Nppb expression to near WT. Reduced fibrosis in BAG3cKO mice, albeit not significantly. partially restored protein expression of FLNC, PINK1, VDAC2, and p62 to amounts similar to WT mice. Significantly reduced the percentage of cardiomyocytes with damaged and reduced sarcomeres in BAG3cKO mice. Significantly reduced mitochondrial content to amounts similar to WT mice.
分子量

434.87

分子式

C15H13ClF2N4O3S2

CAS 番号
Appearance

Solid

Color

White to yellow

SMILES

O=S(N(CC1=NC=C(C2=NN=C(C(F)F)O2)S1)C3=CC(Cl)=CC=C3)(CC)=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 : 100 mg/mL (229.95 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 2.2995 mL 11.4977 mL 22.9954 mL
5 mM 0.4599 mL 2.2995 mL 4.5991 mL
10 mM 0.2300 mL 1.1498 mL 2.2995 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

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Volume
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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

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体積 (開始)

V1

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濃度 (終了)

C2

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体積 (終了)

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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: 2.5 mg/mL (5.75 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2.5 mg/mL.

    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% (20% SBE-β-CD in Saline)

    Solubility: 2.5 mg/mL (5.75 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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 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: 99.84%

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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.2995 mL 11.4977 mL 22.9954 mL 57.4884 mL
5 mM 0.4599 mL 2.2995 mL 4.5991 mL 11.4977 mL
10 mM 0.2300 mL 1.1498 mL 2.2995 mL 5.7488 mL
15 mM 0.1533 mL 0.7665 mL 1.5330 mL 3.8326 mL
20 mM 0.1150 mL 0.5749 mL 1.1498 mL 2.8744 mL
25 mM 0.0920 mL 0.4599 mL 0.9198 mL 2.2995 mL
30 mM 0.0767 mL 0.3833 mL 0.7665 mL 1.9163 mL
40 mM 0.0575 mL 0.2874 mL 0.5749 mL 1.4372 mL
50 mM 0.0460 mL 0.2300 mL 0.4599 mL 1.1498 mL
60 mM 0.0383 mL 0.1916 mL 0.3833 mL 0.9581 mL
80 mM 0.0287 mL 0.1437 mL 0.2874 mL 0.7186 mL
100 mM 0.0230 mL 0.1150 mL 0.2300 mL 0.5749 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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Inquiry Information

製品名:
TYA-018
製品番号:
HY-153392
数量:
MCE 日本正規代理店: