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LY3023703 is a potent, highly selective microsomal prostaglandin E synthase 1 (mPGES1) inhibitor, dose-dependently inhibits PGE2 production in human whole blood ex vivo.
TFC-007, a selective hematopoietic prostaglandin D synthase (H-PGDS) inhibitor, show high inhibitory activity against H-PGDS enzyme (IC50 value of 83 nM). TFC-007 can be used for composing H-PGDS degradation inducer PROTAC(H-PGDS)-1 (TFC-007 binds to H-PGDS, and Pomalidomide binds to cereblon).
AGU654 (Compound 44) is a selective mPGES-1 inhibitor with an IC50 of 2.9 nM against mPGES-1. AGU654 inhibits mPGES-1 to block the pathway converting arachidonic acid into prostaglandin E2 (PGE2) by COX-1/2, thereby alleviating inflammatory responses, pain, and fever. In activated human monocyte-derived macrophages and human whole blood models, AGU654 selectively suppresses bacterial exotoxin-induced PGE2 production while preserving the production of other prostaglandins. In guinea pig models, AGU654 significantly alleviates fever, inflammation, and inflammatory pain, exhibiting excellent anti-inflammatory, analgesic, and antipyretic effects. AGU654 holds promise as a strategy for studying inflammatory diseases and pain.
ADP-β-S (trisodium) is an ADP analog and partial agonist. ADP-β-S (trisodium) induces human platelet aggregation and inhibits PGE1-stimulated adenylate cyclase.
UT-11 is a potent microsomal prostaglandin E synthase-1 (mPGES-1) inhibitor, inhibits PGE2 production from human SK-N-AS and murine BV2 cells induced by LPS with IC50 of 0.1 and 2.0 uM, respectively.
TAS-205 (Pizuglanstat, TAS205) is a potent, specific hematopoietic prostaglandin D synthase (H-PGDS) inhibitor with IC50 of 55.8 nM, does not inhibit LPGDS at 100 uM.
TAS-204 (TAS204) is a potent, specific hematopoietic prostaglandin D synthase (H-PGDS) inhibitor, inhibits recombinant human H-PGDS with IC50 of 24.0 nM.
SZ0232 is a small molecule mPGES-2 (microsomal prostaglandin E synthase-2) inhibitor with IC50 of <1 uM, exhibits beneficial effects on modulating β-cell function and glucose metabolism both in vitro and in vivo.
LY3023703 is a potent, highly selective microsomal prostaglandin E synthase 1 (mPGES1) inhibitor, dose-dependently inhibits PGE2 production in human whole blood ex vivo.
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