Formulation: A solid
Formal Name: 2-ethyl-5,7-dimethyl-3-[[4-[5-(4-piperidinyl)-1,3,4-oxadiazol-2-yl]phenyl]methyl]-pyrazolo[1,5-a]pyrimidine
Purity: ≥98%
Formula Markup: C24H28N6O
Formula Weight: 416,5
Shelf life (days): 1460
CAS Number: 1401728-56-0
Notes: NE52-QQ57 is an antagonist of the G protein-coupled receptor 4 (GPR4; IC50 = 0.04 µM).{68749} It is selective for GPR4 over human-ether-a-go-go (hERG) and histamine H3 receptor (IC50s = 19 and >30 µM, respectively). NE52-QQ57 (2 µM) decreases the IL-33-induced increases in IL-17, IFN-γ, TNF-α, NF-κB, matrix metalloproteinase-2 (MMP-2), MMP-9, and COX-2 levels in, and prostaglandin E2 (PGE2; Item No. 10410) secretion by, HMC-1 mast cells.{68750} It reduces IL-33-induced increases in mitochondrial reactive oxygen species (ROS) in the same cells. NE52-QQ57 (30 mg/kg twice per day) increases colon length and reduces fecal blood levels and incidence of diarrhea, lymph node volumes, and spleen weight, as well as reduces distal and mid colon inflammation and leukocyte infiltration levels, in a mouse model of ulcerative colitis induced by dextran sodium sulfate (DSS).{68751} It increases the mechanical paw withdrawal threshold in a rat model of inflammatory pain induced by complete Freud's adjuvant (CFA) when administered at doses of 3, 10, or 30 mg/kg.{68749}
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