APX-115


Catalog No. Size PriceQuantity
M14150-2 2mg solid $1,940
M14150-10 10mg solid $7,760

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.

Product information

CAS Number: 1395946-75-4

Molecular Weight: 315.80

Formula: C17H18ClN3O

Chemical Name: 3-phenyl-4-propyl-1-(pyridin-2-yl)-1H-pyrazol-5-ol hydrochloride

Smiles: Cl.CCCC1C(=NN(C=1O)C1C=CC=CN=1)C1C=CC=CC=1

InChiKey: GMFJXGGAGPCRBM-UHFFFAOYSA-N

InChi: InChI=1S/C17H17N3O.ClH/c1-2-8-14-16(13-9-4-3-5-10-13)19-20(17(14)21)15-11-6-7-12-18-15;/h3-7,9-12,21H,2,8H2,1H3;1H

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : ≥ 250 mg/mL (791.64 mM).

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

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. In the kidney, APX-115 attenuates Nox gene upregulation and protein expression while improving inflammatory and fibrotic processes.

In Vivo:

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

References:

  1. Kwon G, et al. A novel pan-Nox inhibitor, APX-115, protects kidney injury in streptozotocin-induced diabetic mice: possible role of peroxisomal and mitochondrial biogenesis. Oncotarget. 2017 Jun 16;8(43):74217-74232.
  2. Cha JJ, et al. APX-115, a first-in-class pan-NADPH oxidase (Nox) inhibitor, protects db/db mice from renal injury. Lab Invest. 2017 Apr;97(4):419-431.

Products are for research use only. Not for human use.

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