1. Immunology/Inflammation
  2. PGE synthase
  3. AT-56

AT-56 is a potent, selective and orally active inhibitor of lipocalin-type prostaglandin D synthase (L-PGDS), with an IC50 of 95 μM and Ki of 75 μM. AT-56 could selectively suppress the drowsiness or pain reaction mediated by L-PGDS-catalyzed PGD2.

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AT-56

AT-56 構造式

CAS 番号 : 162640-98-4

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 104 在庫あり
Solution
10 mM * 1 mL in DMSO USD 104 在庫あり
Solid
5 mg $95 在庫あり
10 mg $160 在庫あり
25 mg $320 在庫あり
50 mg $510 在庫あり
100 mg $800 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

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製品説明

AT-56 is a potent, selective and orally active inhibitor of lipocalin-type prostaglandin D synthase (L-PGDS), with an IC50 of 95 μM and Ki of 75 μM. AT-56 could selectively suppress the drowsiness or pain reaction mediated by L-PGDS-catalyzed PGD2[1].

IC50 & Target

IC50: 95 μM (L-PGDS); Ki: 75 μM (L-PGDS)[1]

体外実験

AT-56 (1-30 μM; 10 minutes) dose-dependently inhibits the production of PGD2 in L-PGDS-expressing human medulloblastoma TE-671 cells with an IC50 of about 3 μM[1].

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

体内実験

AT-56 (?1-30 mg/kg; p.o.) suppresses the PGD2 production in the stab-wounded brain[1].
AT-56 (1-10 mg/kg; p.o.) suppresses the L-PGDS-mediated allergic airway inflammation in mice[1].
AT-56 (10 mg/kg; p.o.) exhibits Cmax (2.15 μg/ml), half-life (1.71 h) and high oral bioavailability (82%)[1].

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

Animal Model: H-PGDS KO mice (14-16weeks, 25-30 g, C57BL/6 strain) with a stab wound brain injury[1]
Dosage: 0, 1, 3, 10, 30 mg/kg
Administration: P.o. 1 h before the stab wound injury
Result: Inhibited the L-PGDS reaction in the brain.
Decreased the total amount of PGD2 in the brain to 40% with 30 mg/kg AT-56.
Animal Model: Human L-PGDS-overexpressing TG mice (males, 14-16 weeks, 25-30 g)[1]
Dosage:  0, 1, 10 mg/kg
Administration: P.o. 1 h before and 24 h after the antigen exposure
Result: Prevented the eosinophil infiltration by inhibiting transgened human L-PGDS.
Animal Model: Male C57BL/6 mice (7 weeks, 22-26 g)[1]
Dosage: 10 mg/kg for p.o. and 2 mg/kg for i.v. (Pharmacokinetic Analysis)
Administration: P.o. and i.v. administration
Result: Oral bioavailability (82%); Cmax (2.15 μg/ml); T1/2 (1.71 h, p.o.); T1/2 (2.35 h, i.v.).
分子量

397.52

分子式

C25H27N5

CAS 番号
Appearance

Solid

Color

White to off-white

SMILES

N1(CCCCC2=NNN=N2)CC/C(CC1)=C3C4=CC=CC=C4C=CC5=CC=CC=C/35

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件
Powder -20°C 3 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

DMSO : 100 mg/mL (251.56 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 2.5156 mL 12.5780 mL 25.1560 mL
5 mM 0.5031 mL 2.5156 mL 5.0312 mL
10 mM 0.2516 mL 1.2578 mL 2.5156 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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一般には略語で表示されます:C1V1 = C2V2

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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 (6.29 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% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (6.29 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 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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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: 99.75%

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 2.5156 mL 12.5780 mL 25.1560 mL 62.8899 mL
5 mM 0.5031 mL 2.5156 mL 5.0312 mL 12.5780 mL
10 mM 0.2516 mL 1.2578 mL 2.5156 mL 6.2890 mL
15 mM 0.1677 mL 0.8385 mL 1.6771 mL 4.1927 mL
20 mM 0.1258 mL 0.6289 mL 1.2578 mL 3.1445 mL
25 mM 0.1006 mL 0.5031 mL 1.0062 mL 2.5156 mL
30 mM 0.0839 mL 0.4193 mL 0.8385 mL 2.0963 mL
40 mM 0.0629 mL 0.3144 mL 0.6289 mL 1.5722 mL
50 mM 0.0503 mL 0.2516 mL 0.5031 mL 1.2578 mL
60 mM 0.0419 mL 0.2096 mL 0.4193 mL 1.0482 mL
80 mM 0.0314 mL 0.1572 mL 0.3144 mL 0.7861 mL
100 mM 0.0252 mL 0.1258 mL 0.2516 mL 0.6289 mL
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  • Molarity Calculator

  • Dilution Calculator

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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:
AT-56
製品番号:
HY-13988
数量:
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