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1-Benzyl-N5-cyclopropyl-N3-methyl-2-oxo-1,2-dihydropyridine-3,5-dicarboxamide, GSK 620, GSK-620, N5-Cyclopropyl-1,2-dihydro-N3-methyl-2-oxo-1-(phenylmethyl)-3,5-pyridinedicarboxamide
C18H19N3O3
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Quality Level
Assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
2-8°C
SMILES string
O=C1N(C=C(C=C1C(NC)=O)C(NC2CC2)=O)CC3=CC=CC=C3
Biochem/physiol Actions
GSK620 Is an orally active, potent and selective pan-second bromodomain (BD2) inhibitor (BD2/BD1 pIC50 = 6.5/4.6/BRD2, 7.1/4.6/BRD3, 7.1/4.8/BRD4, 6.7/4.6/BRDT) with improved oral availability than GSK046 (iBET-BD2) and in vivo efficacy in inflammatory disease models, including collagen-induced arthritis (3-10 mg/kg/d p.o. in rats), imiquimod (IMQ)-induced psoriasis (20 mg/kg/d p.o. in mice), and a nonalcoholic steatohepatitis (NAFLD) model (20 mg/kg/d p.o. in STAM mice).
WGK
WGK 3
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
Regulatory Information
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Certificates of Analysis (COA)
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