GKT136901 hydrochloride

CAS No. 1254507-01-1

GKT136901 hydrochloride( —— )

Catalog No. M35054 CAS No. 1254507-01-1

GKT136901 hydrochloride is a NOX-1/4 inhibitor, a selective scavenger of peroxynitrite, which inhibits METH-induced ROS production.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    GKT136901 hydrochloride
  • Note
    Research use only, not for human use.
  • Brief Description
    GKT136901 hydrochloride is a NOX-1/4 inhibitor, a selective scavenger of peroxynitrite, which inhibits METH-induced ROS production.
  • Description
    GKT136901 hydrochloride is a potent, selective and orally active inhibitor of NADPH oxidase (NOX1/4), with Kis of 160 and 165 nM, respectively. GKT136901 hydrochloride is also a selective and direct scavenger of peroxynitrite. GKT136901 hydrochloride can be used for the research of diabetic nephropathy, stroke, and neurodegeneration. GKT136901 hydrochloride also has anti-inflammatory activity.
  • In Vitro
    ——
  • In Vivo
    Animal Model:Male db/db and db/m mice (8 weeks)Dosage:30, 90 mg/kg Administration:Daily p.o. for 16 weeksResult:Reduced albuminuria, thiobarbituric acid-reacting substances (TBARS) and renal ERK1/2 phosphorylation and preserved renal structure in diabetic mice.Had no effect on plasma glucose, BP (blood pressure), and body weight.
  • Synonyms
    ——
  • Pathway
    Membrane Transporter/Ion Channel
  • Target
    NADPH
  • Recptor
    NADPH-oxidase
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    1254507-01-1
  • Formula Weight
    403.26
  • Molecular Formula
    C19H16Cl2N4O2
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : 62.5 mg/mL (154.99 mM; Ultrasonic ) H2O : 4 mg/mL (9.92 mM; Ultrasonic (<60°C))
  • SMILES
    Cl.O=C1C=C2NN(C(=O)C2=C(N1CC3=NC=CC=C3)C)C=4C=CC=CC4Cl
  • Chemical Name
    ——

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Laleu B, et, al. First in class, potent, and orally bioavailable NADPH oxidase isoform 4 (Nox4) inhibitors for the treatment of idiopathic pulmonary fibrosis. J Med Chem. 2010 Nov 11;53(21):7715-30.?
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