1. Metabolic Enzyme/Protease
  2. FABP
  3. HTS01037

HTS01037 is an inhibitor of fatty acid binding; and a competitive antagonist of protein-protein interactions mediated by AFABP/aP2 with a Ki of 0.67 μM.

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HTS01037

HTS01037 構造式

CAS 番号 : 682741-29-3

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 92 在庫あり
Solution
10 mM * 1 mL in DMSO USD 92 在庫あり
Solid
5 mg $84 在庫あり
10 mg $144 在庫あり
25 mg $312 在庫あり
50 mg $500 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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カスタマーレビュー

Based on 1 publication(s) in Google Scholar

Other Forms of HTS01037:

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

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製品説明

HTS01037 is an inhibitor of fatty acid binding; and a competitive antagonist of protein-protein interactions mediated by AFABP/aP2 with a Ki of 0.67 μM.

IC50 & Target

IC50: 0.67 μM (AFABP/aP2)[1]

体外実験

HTS01037 functions as a high affinity ligand of AFABP/aP2 with an apparent Ki of 0.67 μM. HTS01037 is somewhat selective for AFABP/aP2, but at higher concentrations is a pan-specific FABP inhibitor. HTS01037 inhibits lipolysis in 3T3-L1 adipocytes and reduces LPS-stimulated inflammation in cultured macrophages. HTS01037 acts as an antagonist of the protein-protein interaction between AFABP/aP2 and hormone sensitive lipase but does not activate PPARγ in macrophage or CV-1 cells[1]. Treatment of microglial cells with HTS01037 increases expression of Ucp2 and arginase in the presence or absence of palmitic acid. Moreover, cells exposed to HTS01037 exhibits attenuated expression of inducible nitric oxide synthase (iNOS) compared to palmitic acid alone indicating reduced NFκB signaling[2]. Treatment of macrophages with HTS01037results in a marked decrease in both basal and fatty acid-stimulated LTC4 secretion but no change in 5-HETE production or 5-lipoxygenase expression[3].

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

分子量

337.37

分子式

C14H11NO5S2

CAS 番号
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(C1=C(NC(/C=C/C(O)=O)=O)C=C(C2=CC=CS2)S1)OC

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 (296.41 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 2.9641 mL 14.8205 mL 29.6410 mL
5 mM 0.5928 mL 2.9641 mL 5.9282 mL
10 mM 0.2964 mL 1.4821 mL 2.9641 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
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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

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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 (7.41 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 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 (7.41 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

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
参考文献
キナーゼ実験
[1]

To analyze the ligand (HTS01037) binding properties of the FABPs, the fluorescent ligand 1-anilinonapthalene 8-sulfonic acid (1,8-ANS) is utilized. 1,8 ANS is dissolved in absolute ethanol and diluted with 25 mM Tris-HCl (pH 7.4) to a final concentration of 5 μM (final EtOH concentration of 0.05%). Protein is titrated into 500 μL 1,8-ANS and the fluorescence enhancement is measured using a Perkin Elmer 650-10S fluorescence spectrophotometer with 4 nm excitation and emission slit widths. Quantitative analysis of ligand binding is evaluated using non-linear regression using PRISM software[1].

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。

細胞実験
[2]

Cells are pretreated with HTS01037 or vehicle for 3 h and then challenged with or without palmitic acid for 1 h. Cells are then exposed to the ROS Deep Red Dye for 1 h in 5% CO2 at 37°C. Intracellular superoxide and hydroxyl radicals react with the deep red dye, producing a fluorescent signal which is measured using a spectrophotometer at 650Ex/675Em[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 2.9641 mL 14.8205 mL 29.6410 mL 74.1026 mL
5 mM 0.5928 mL 2.9641 mL 5.9282 mL 14.8205 mL
10 mM 0.2964 mL 1.4821 mL 2.9641 mL 7.4103 mL
15 mM 0.1976 mL 0.9880 mL 1.9761 mL 4.9402 mL
20 mM 0.1482 mL 0.7410 mL 1.4821 mL 3.7051 mL
25 mM 0.1186 mL 0.5928 mL 1.1856 mL 2.9641 mL
30 mM 0.0988 mL 0.4940 mL 0.9880 mL 2.4701 mL
40 mM 0.0741 mL 0.3705 mL 0.7410 mL 1.8526 mL
50 mM 0.0593 mL 0.2964 mL 0.5928 mL 1.4821 mL
60 mM 0.0494 mL 0.2470 mL 0.4940 mL 1.2350 mL
80 mM 0.0371 mL 0.1853 mL 0.3705 mL 0.9263 mL
100 mM 0.0296 mL 0.1482 mL 0.2964 mL 0.7410 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:
HTS01037
製品番号:
HY-101503
数量:
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