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Chemical Structure| 1270084-92-8 Chemical Structure| 1270084-92-8

Structure of APX-115 free base
CAS No.: 1270084-92-8

Chemical Structure| 1270084-92-8

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APX-115 free base (Ewha-18278 free base) 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.

Synonyms: Ewha-18278 free base; Isuzinaxib free base; EWHA-18278

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Product Details of APX-115 free base

CAS No. :1270084-92-8
Formula : C17H17N3O
M.W : 279.34
SMILES Code : OC1=C(CCC)C(C2=CC=CC=C2)=NN1C3=NC=CC=C3
Synonyms :
Ewha-18278 free base; Isuzinaxib free base; EWHA-18278
MDL No. :N/A
InChI Key :GIWZEELPLKPYBA-UHFFFAOYSA-N
Pubchem ID :51036475

Safety of APX-115 free base

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P264-P271-P280-P302+P352-P304+P340+P312-P305+P351+P338-P332+P313-P337+P313-P403+P233-P405-P501

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
primary chondrocytes 10 µM 24 h APX-115 significantly decreased IL-1β-induced ROS production and oxidative DNA damage, and most potently suppressed the expression of oxidative stress marker genes and catabolic proteases. Antioxidants (Basel). 2022 Nov 27;11(12):2346
Murine mesangial cells (MES-13) 1 µM 30 min To evaluate the effect of APX-115 on high glucose and angiotensin II-induced intracellular ROS generation. Results showed that APX-115 significantly inhibited high glucose and angiotensin II-induced ROS generation. Oncotarget. 2017 Jun 16;8(43):74217-74232

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
C57BL/6 mice Surgically induced osteoarthritis model by destabilization of the medial meniscus (DMM) Intraperitoneal injection 60 mg/kg Twice a week for 8 weeks APX-115 significantly attenuated the severity of surgically induced osteoarthritis, reducing cartilage damage and the expression of oxidative DNA damage marker 8-oxo-dG. Antioxidants (Basel). 2022 Nov 27;11(12):2346
C57BL/6J mice Aging diabetic model Oral gavage 60 mg/kg Once daily for 12 weeks APX-115 significantly improved insulin resistance in diabetic aging mice, reduced urinary excretion of the oxidative stress marker 8-isoprostane, and ameliorated mesangial expansion, macrophage infiltration, and expression of fibrotic molecules. Additionally, APX-115 decreased the protein expression of Nox1, Nox2, and Nox4 in the kidney and restored Klotho expression levels. Kidney Res Clin Pract. 2024 Nov;43(6):763-773
C57BL/6J mice Streptozotocin (STZ)-induced type 1 diabetic mouse model Oral 60 mg/kg Once daily for 12 weeks To evaluate the protective effect of APX-115 on diabetic kidney injury. Results showed that APX-115 significantly reduced urinary albumin excretion, glomerular hypertrophy, tubular injury, podocyte injury, fibrosis, and inflammation, and inhibited oxidative stress. Additionally, APX-115 restored mitochondrial and peroxisomal biogenesis in diabetic kidneys. Oncotarget. 2017 Jun 16;8(43):74217-74232

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.58mL

0.72mL

0.36mL

17.90mL

3.58mL

1.79mL

35.80mL

7.16mL

3.58mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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