1. Metabolic Enzyme/Protease
  2. Phosphodiesterase (PDE)
  3. Enpp-1-IN-12

Enpp-1-IN-12 (compound 43) is a potent and orally active ecto-nucleotide pyrophosphatase/phosphodiesterases 1 (ENPP1) inhibitor, with a Ki of 41 nM. Enpp-1-IN-12 exhibits anti-tumor activity.

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Enpp-1-IN-12

Enpp-1-IN-12 構造式

CAS 番号 : 2631703-41-6

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 374 在庫あり
Solution
10 mM * 1 mL in DMSO USD 374 在庫あり
Solid
5 mg $340 在庫あり
10 mg $580 在庫あり
25 mg $1150 在庫あり
50 mg $1850 在庫あり
100 mg $2950 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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Phosphodiesterase (PDE) アイソフォーム固有の製品をすべて表示:

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製品説明

Enpp-1-IN-12 (compound 43) is a potent and orally active ecto-nucleotide pyrophosphatase/phosphodiesterases 1 (ENPP1) inhibitor, with a Ki of 41 nM. Enpp-1-IN-12 exhibits anti-tumor activity[1].

IC50 & Target

Ki: 41 nM (ENPP1)[1]

体外実験

Enpp-1-IN-12 (5 μM) exhibits half-life and intrinsic clearance of >120 min and <11.55 μL/min/million cells and 61.88 min and 22.4 μL/min/million cells in human and mouse hepatocytes, respectively[1].

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

体内実験

Enpp-1-IN-12 (100 mg/kg; p.o.) inhibits tumor growth in LLC1 syngeneic murine tumor model for lung cancer[1].
Enpp-1-IN-12 (10 mg/kg; p.o.) exhibits moderate oral bioavailability (F=45.1%), half-life (t1/2=1.04 h), and Cmax (303.10 ng/mL) in healthy female BALB/c mice[1].
Enpp-1-IN-12 (1 mg/kg; i.v.) exhibits half-life (t1/2=0.76 h), Cmax (308.64 ng/mL), and CL of 73.22 mL/min/kg in healthy female BALB/c mice[1].

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

分子量

374.42

分子式

C16H18N6O3S

CAS 番号
Appearance

Solid

Color

Off-white to gray

SMILES

O=C(C(CC)SC1=NC(N)=NC2=C1NC=N2)NC3=CC=C(C(OC)=C3)O

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

溶剤 & 溶解度
体外: 

DMSO : 50 mg/mL (133.54 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 2.6708 mL 13.3540 mL 26.7080 mL
5 mM 0.5342 mL 2.6708 mL 5.3416 mL
10 mM 0.2671 mL 1.3354 mL 2.6708 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 (sealed storage, away from moisture and light). 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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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

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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: ≥ 1 mg/mL (2.67 mM); Clear solution

    This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 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% Corn Oil

    Solubility: ≥ 1 mg/mL (2.67 mM); Clear solution

    This protocol yields a clear solution of ≥ 1 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 (10.0 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).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

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: 99.28%

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 (sealed storage, away from moisture and light). 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 2.6708 mL 13.3540 mL 26.7080 mL 66.7699 mL
5 mM 0.5342 mL 2.6708 mL 5.3416 mL 13.3540 mL
10 mM 0.2671 mL 1.3354 mL 2.6708 mL 6.6770 mL
15 mM 0.1781 mL 0.8903 mL 1.7805 mL 4.4513 mL
20 mM 0.1335 mL 0.6677 mL 1.3354 mL 3.3385 mL
25 mM 0.1068 mL 0.5342 mL 1.0683 mL 2.6708 mL
30 mM 0.0890 mL 0.4451 mL 0.8903 mL 2.2257 mL
40 mM 0.0668 mL 0.3338 mL 0.6677 mL 1.6692 mL
50 mM 0.0534 mL 0.2671 mL 0.5342 mL 1.3354 mL
60 mM 0.0445 mL 0.2226 mL 0.4451 mL 1.1128 mL
80 mM 0.0334 mL 0.1669 mL 0.3338 mL 0.8346 mL
100 mM 0.0267 mL 0.1335 mL 0.2671 mL 0.6677 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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製品名:
Enpp-1-IN-12
製品番号:
HY-143256
数量:
MCE 日本正規代理店: