Zaloglanstat (ISC-27864) is a potent inhibitor of microsomal prostaglandin E synthase-1 (mPGES-1). It is utilized in the research of various conditions, including asthma, osteoarthritis, rheumatoid arthritis, acute or chronic pain, and neurodegenerative diseases.
Vipoglanstat is a prostaglandin E synthase inhibitor and an anti-inflammatory. Vipoglanstat ameliorates leukocyte infiltration and lung injury resulting from both endotoxin-induced and sepsis-induced lung injury.
AF3442 is a potent and selective mPGES-1 inhibitor (microsomal prostaglandin (PG) E synthase-1). AF3442 caused a concentration-dependent inhibition of PGE(2) in human recombinant mPGES-1 with an IC(50) of 0.06microM. AF3442 is a selective mPGES-1 inhibitor which reduced monocyte PGE(2) generation also in the presence of plasma proteins. Pharmacological inhibition of mPGES-1 did not translate into redirection of PGH(2) metabolism towards other terminal PG synthases in monocytes. The functional relevance of this observation deserves to be investigated in vivo.
PF-4693627 is an effective and selective microsomal prostaglandin E synthase-1 inhibitor (IC50=3 nM). It is used for the treatment of inflammation caused by osteoarthritis (OA) and rheumatoid arthritis (RA).
(±)-γ-Tocopherol is a form of vitamin E with antioxidant and anti-inflammatory properties. It traps and detoxifies reactive nitrogen oxide species, including nitrogen dioxide, in cell-free assays. It also reduces the synthesis of prostaglandin E2 (PGE2) induced by LPS in RAW 264.7 macrophages and by IL-1β in A549 cells. (±)-γ-Tocopherol inhibits LPS-induced nitrite release and inducible nitric oxide synthase (iNOS) expression in RAW 264.7 cells and reduces COX-2 activity in A549 cells pretreated with IL-1β. Serum levels of (±)-γ-tocopherol are decreased in patients with cardiovascular disease.
Prostaglandin D2 (PGD2) is one of the five principal prostaglandins enzymatically derived from PGH2. It is abundantly generated in the cerebrospinal fluid (CSF) by lipocalin-type PGD synthase and in peripheral regions by myeloid cells, such as mast cells and basophils, via leukocyte-type PGD synthase. The compound 1,25-trans-PGD2 is an isomer of PGD2, characterized by the alteration of the double bond between carbons 5 and 6 from cis(Z) to trans(E). This trans isomer, found as a 2-5% impurity in most commercial PGD2 bulk drug preparations, is primarily synthesized as an analytical standard to identify and quantify this impurity. Based on existing studies of trans isomers of F-type prostaglandins, 5-trans-PGD2 likely exhibits biological activity comparable to its cis isomer, although no specific published reports confirm this for 5-trans-PGD2.