1. Neuronal Signaling
  2. Transthyretin (TTR)
  3. Acoramidis

Acoramidis (AG10) is an orally active and selective kinetic stabilizer of WT and V122I-TTR (transthyretin). Acoramidis (AG10) is used in the study for transthyretin amyloidosis.

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Acoramidis

Acoramidis 構造式

CAS 番号 : 1446711-81-4

容量 価格(税別) 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 165 在庫あり
Solution
10 mM * 1 mL in DMSO USD 165 在庫あり
Solid
1 mg $60 在庫あり
5 mg $150 在庫あり
10 mg $250 在庫あり
25 mg $400 在庫あり
50 mg $588 在庫あり
100 mg $920 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

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製品説明

Acoramidis (AG10) is an orally active and selective kinetic stabilizer of WT and V122I-TTR (transthyretin). Acoramidis (AG10) is used in the study for transthyretin amyloidosis[1][2].

体外実験

Acoramidis (AG10, 0.1-10 μM for TTR ~5 μM) stabilizes V122I- and WT-TTR equally well and also exceeds their efficacy to stabilize WT and mutant TTR in whole serum[1].
Acoramidis (AG10) stimulates the mitochondrial QO2 in a concentration-dependent manner between 10 and 100 μM[3].
Acoramidis (AG10) has very minimal inhibition of two common off-targets in drug discovery, the potassium ion channel hERG (IC50 > 100 μM) and a number of cytochrome P450 isozymes (IC50 > 50 μM) (low toxicity)[1].

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

Western Blot Analysis[1].

Cell Line: Human serum (TTR ∼5 µM).
Concentration: 0.1 and 10 μM.
Incubation Time: 72 h.
Result: Was significantly more effective than tafamidis in stabilizing TTR.
The concentration of AG10 to 10 µM resulted in stabilization of almost all of TTR in serum.
体内実験
Animal Model: Wistar rats[1].
Dosage: 50 mg/kg/d (Toxicity Analysis).
Administration: Oral gavage, daily for 28 d.
Result: Showed the plasma Cmax of ∼40 µM and histopathological evaluation of liver, kidney, heart, spleen, thymus, and lung showed no signs of pathologic processes in the AG10-treated animals
臨床実験
分子量

292.31

分子式

C15H17FN2O3

CAS 番号
Appearance

Solid

Color

White to off-white

SMILES

O=C(O)C1=CC=C(F)C(OCCCC2=C(C)NN=C2C)=C1

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 (342.10 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 3.4210 mL 17.1051 mL 34.2103 mL
5 mM 0.6842 mL 3.4210 mL 6.8421 mL
10 mM 0.3421 mL 1.7105 mL 3.4210 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.

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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 (8.55 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 (8.55 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 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:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
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+
%
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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
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 3.4210 mL 17.1051 mL 34.2103 mL 85.5256 mL
5 mM 0.6842 mL 3.4210 mL 6.8421 mL 17.1051 mL
10 mM 0.3421 mL 1.7105 mL 3.4210 mL 8.5526 mL
15 mM 0.2281 mL 1.1403 mL 2.2807 mL 5.7017 mL
20 mM 0.1711 mL 0.8553 mL 1.7105 mL 4.2763 mL
25 mM 0.1368 mL 0.6842 mL 1.3684 mL 3.4210 mL
30 mM 0.1140 mL 0.5702 mL 1.1403 mL 2.8509 mL
40 mM 0.0855 mL 0.4276 mL 0.8553 mL 2.1381 mL
50 mM 0.0684 mL 0.3421 mL 0.6842 mL 1.7105 mL
60 mM 0.0570 mL 0.2851 mL 0.5702 mL 1.4254 mL
80 mM 0.0428 mL 0.2138 mL 0.4276 mL 1.0691 mL
100 mM 0.0342 mL 0.1711 mL 0.3421 mL 0.8553 mL
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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)
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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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Inquiry Information

製品名:
Acoramidis
製品番号:
HY-109165
数量:
MCE 日本正規代理店: