Formulation: A solid
Formal Name: 2-bromo-N-(5-(3'-hydroxy-[1,1'-biphenyl]-4-yl)-1,3,4-thiadiazol-2-yl)benzamide
Purity: ≥95%
Formula Markup: C21H14BrN3O2S
Formula Weight: 452,3
Shelf life (days): 1095
Notes: Prostaglandin E2 (PGE2) inhibitor 3 is an inhibitor of microsomal prostaglandin E synthase-1 (mPGES-1; IC50 = 0.2 µM).{51389} It is selective for mPGES-1 over COX-1, COX-2, 5-lipoxygenase (5-LO), and soluble epoxide hydrolase (sEH) in cell-free assays at 10 µM. PGE2 inhibitor 3 inhibits IL-1β-induced production of PGE2 (Item No. 14010) in A549 cells and LPS-induced IL-6 and PGE2 production in J774A.1 macrophages when used at concentrations of 10 and 1 µM, respectively. It also inhibits the formation of 5-LO products, including leukotriene B4 (LTB4; Item No. 20110) and 5-H(p)ETE, induced by the calcium ionophore A23187 (Item Nos. 11016 / 22030) alone or with arachidonic acid (Item Nos. 90010 / 90010.1 / 10006607) and A23187 (IC50s = 4.9 and 5.2 µM, respectively). In vivo, PGE2 inhibitor 3 (10 mg/kg) prevents leukocyte infiltration into the peritoneal fluid in a mouse model of zymosan-induced peritonitis.
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