1. Metabolic Enzyme/Protease
  2. NADPH Oxidase
  3. APX-115

APX-115  (Synonyms: Ewha-18278)

Cat. No.: HY-120801 Purity: 99.58%
SDS COA Handling Instructions

APX-115 (Ewha-18278) is a potent, orally active pan NADPH oxidase (Nox) inhibitor with Ki values of 1.08 μM, 0.57 μM, and 0.63 μM for Nox1, Nox2 and Nox4, respectively. APX-115 effectively prevents kidney injury.

For research use only. We do not sell to patients.

APX-115 Chemical Structure

APX-115 Chemical Structure

CAS No. : 1395946-75-4

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Customer Review

Based on 1 publication(s) in Google Scholar

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1 Publications Citing Use of MCE APX-115

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

APX-115 (Ewha-18278) is a potent, orally active pan NADPH oxidase (Nox) inhibitor with Ki values of 1.08 μM, 0.57 μM, and 0.63 μM for Nox1, Nox2 and Nox4, respectively. APX-115 effectively prevents kidney injury[1].

IC50 & Target

NOX1

 

NOX2

 

NOX4

 

In Vitro

APX-115 (5 μM; 60 min) almost completely suppresses high glucose-induced proinflammatory and profibrotic molecule expression in the mouse podocyte cell line[2].
In the kidney, APX-115 attenuates Nox gene upregulation and protein expression while improving inflammatory and fibrotic processes[2].

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

In Vivo

APX-115 (oral gavage; 60 mg/kg/day; for 12 weeks) significantly improves insulin resistance in diabetic mice[2].
APX-115 treatment decreases the urinary excretion of albumin and plasma creatinine levels[2].

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

Animal Model: Six-week-old male diabetic db/db mice (C57BLKS/J-leprdb/leprdb)[2]
Dosage: 60 mg/kg
Administration: Oral gavage; per day; for 12 weeks
Result: Significantly improved insulin resistance in diabetic mice.
Clinical Trial
Molecular Weight

315.80

Formula

C17H18ClN3O

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

OC1=C(CCC)C(C2=CC=CC=C2)=NN1C3=NC=CC=C3.Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

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

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (316.66 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 3.1666 mL 15.8328 mL 31.6656 mL
5 mM 0.6333 mL 3.1666 mL 6.3331 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). 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)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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: ≥ 2.08 mg/mL (6.59 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (6.59 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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).

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

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.
Purity & Documentation

Purity: 99.58%

References

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). 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 3.1666 mL 15.8328 mL 31.6656 mL 79.1640 mL
5 mM 0.6333 mL 3.1666 mL 6.3331 mL 15.8328 mL
10 mM 0.3167 mL 1.5833 mL 3.1666 mL 7.9164 mL
15 mM 0.2111 mL 1.0555 mL 2.1110 mL 5.2776 mL
20 mM 0.1583 mL 0.7916 mL 1.5833 mL 3.9582 mL
25 mM 0.1267 mL 0.6333 mL 1.2666 mL 3.1666 mL
30 mM 0.1056 mL 0.5278 mL 1.0555 mL 2.6388 mL
40 mM 0.0792 mL 0.3958 mL 0.7916 mL 1.9791 mL
50 mM 0.0633 mL 0.3167 mL 0.6333 mL 1.5833 mL
60 mM 0.0528 mL 0.2639 mL 0.5278 mL 1.3194 mL
80 mM 0.0396 mL 0.1979 mL 0.3958 mL 0.9896 mL
100 mM 0.0317 mL 0.1583 mL 0.3167 mL 0.7916 mL
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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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APX-115
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HY-120801
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