SML2770

GSK2795039

≥98% (HPLC)

• Synonym(s): GSK 2795039, GSK-2795039, N-(1-Isopropyl-3-(1-methylindolin-6-yl)-1H-pyrrolo[2,3-b]pyridin-4-yl)-1-methyl-1H-pyrazole-3-sulfonamide
• Empirical Formula (Hill Notation): C₂₃H₂₆N₆O₂S
• CAS Number: 1415925-18-6
• Molecular Weight: 450.56
• MDL number: MFCD30489720
• UNSPSC Code: 12352200
• NACRES: NA.77

Properties

• Quality Level: 100
• Assay: ≥98% (HPLC)
• form: powder
• color: white to beige
• solubility: DMSO: 2 mg/mL, clear
• storage temp.: −20°C
• SMILES string: O=S(NC1=C2C(N(C(C)C)C=C2C3=CC4=C(C=C3)CCN4C)=NC=C1)(C5=NN(C)C=C5)=O
• InChI key: FMWVTCZKCXPKFW-UHFFFAOYSA-N

Description

Biochem/physiol Actions

GSK2795039 is a non-cytotoxic (100 μM, 24 hrs, HEK293), NADPH-competitive, potent and selective NOX2 inhibitor (IC₅₀/[NADPH] = 447 nM/25 μM, 2.29 μM/1 mM by NADPH depletion measurement; eNOS & NOX1/3/4/5 IC₅₀ >100 μM, PKCB II IC₅₀ >25 μM, xanthine oxidase IC₅₀ = 28.8 μM). GSK2795039 inhibits PMA-induced reactive oxygen species (ROS) production in cultures (IC₅₀ = 182 nM; HL60) and exhibits in vivo efficacy against complete Freund′s adjuvant-induced paw inflammation (ED₅₀ = 2 mg/kg, ED₁₀₀ = 100 mg/kg ip.) as well as cerulein-induced acute pancreatitis (ED₅₀ = 100 mg/kg ip.) in mice.

NADPH-competitive, potent and selective NOX2 inhibitor with in vitro and in vivo efficacy against NOX2-mediated ROS production and inflammation.

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3