Setanaxib

SKU: orb1301074

Description

Setanaxib

Research Area

Cell Biology, Immunology & Inflammation, Metabolism Research

Key Properties

• CAS Number: 1218942-37-0
• MW: 394.85
• Purity: 99.66%
• Formula: C₂₁H₁₉ClN₄O₂
• SMILES: CN(C)c1cccc(c1)-c1n(C)c(=O)cc2[nH]n(-c3ccccc3Cl)c(=O)c12
• Target: Ferroptosis,NADPH,NADPH-oxidase
• Solubility: Ethanol:< 1 mg/mL (insoluble or slightly soluble);10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (2.53 mM);DMSO:125 mg/mL (316.58 mM)

Bioactivity

• Target IC50:
  NOX4:140 nM(Ki)|NOX1:110 nM(Ki)
• In Vivo:
  GKT137831 can prevent oxidative stress in human aortic endothelial cells in response to hyperglycemia. It attenuate the release of H2O2, cellular proliferation, and TGF-β1 expression induced by hypoxia in HPAECs and HPASMCs, while also amelioratin the reduction in PPARγ expression.
• In Vitro:
  Administering 60 mg/kg of GKT137831 orally every day to mice models living in a chronic hypoxic envir nMent mitigates long-term hypoxia-induced right ventricular hypertrophy, vascular remodeling, pulmonary cell proliferation, and alter the expression of pulmonary PPARγ and TGF-β. Similarly, daily oral administration of 60 mg/kg GKT137831 to atherosclerotic mice deficient in apolipoprotein E (ApoE) under diabetic conditions attenuates accelerated arteriosclerosis. Additionally, GKT137831 at a dosage of 60 mg/kg i.g. block the progression of liver fibrosis In both WT and SOD1mut mice, and reduces oxidative stress, inflammation, and fibrogenesis. furthermore , in AngII-infused c-hNox4Tg mice, GKT137831 eradicate the increase in oxidative stress, inhibit the Akt-mTOR and NF-κB signaling pathways, and diminishes cardiac remodeling.
• Cell Research:
  Hypoxic HPASMC and HPAEC proliferation is determined using MTT assay, by Western blotting to detect proliferating cell nuclear antigen (PCNA) expression, or by manual cell counting after Trypan blue staining. Amplex Red Hydrogen Peroxide/Peroxidase Assay Kit is used to measure Water2 released int the culture media from HPAECs or HPASMCs. After exposure to control or hypoxic envir nMents for 72 hours, Amplex Red reagent is added, an the cells are returned to control or hypoxic envir nMents for an additional hour before fluorescence measurements. (Only for Reference)

Storage & Handling

• Storage: store at low temperature,keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Ferroptosis, GKT 137831, GKT 831, GKT137831, GKT-137831, GKT831, GKT-831, Inhibitor, NOX, NOX1, NOX4, inhibit, NADPH Oxidase, NADPHoxidase, Setanaxib

Compound Identifiers

PubChem CID

58496428