PGE synthase Inhibitor

mPGES-1/5-LOX-IN-1 (compound 3j) is a potent and orally active mPGES-1 and 5-LOX dual inhibitor with IC₅₀ values of 0.92, 1.89 µM, respectively. mPGES-1/5-LOX-IN-1 shows anti-inflammatory impact.

MDL 19301 is a nonsteroidal, anti-inflammatory agent.

AF3442 is a potent and selective mPGES-1 inhibitor (IC₅₀ = 0.06 μM) which reduces monocyte PGE₂ generation also in the presence of plasma proteins. AF3442 shows selectivity over other prostanoids (TXB₂, PGF_2α and 6-keto-PGF_1α). AF3442 can be used for research in analgesia.

5-trans U-44069 is the trans isomer of the thromboxane receptor agonist U-44069 (HY-121825). 5-trans U-44069 inhibits prostaglandin E2 synthase activity.

AGU661 is a Microsomal prostaglandin E2 synthase 1 (mPGES-1) inhibitor with an IC₅₀ of 0.22  nM. AGU661 lowers PGE2 formation in human pro-inflammatory M1 macrophages and activated monocytes without affecting other lipid mediator pathways. AGU661 has unfavorable physicochemical properties with poor metabolic stability and strong plasma protein binding tendencies. AGU661 into PLGA-based NPs significantly enhances its bioactivity. AGU661 can be used for inflammatory disorders research.

mPGES1-IN-5 (compound 18) is a polysubstituted pyrimidine compound and a submicromolar PGE2 production inhibitor. It exerts its anti-inflammatory effect mainly by inhibiting mPGES-1 and has a significant inhibitory effect on the acute inflammation model in vivo.

Benoxaprofen-¹³C, d₃ is the ¹³C-labeled Benoxaprofen (HY-13568). Benoxaprofen (LRCL 3794) is a nonsteroidal anti-inflammatory agent that blocks the biosynthesis of inflammatory mediators such as leukotrienes and prostaglandins by inhibiting 5-LOX, PGH2 synthase and cytochrome P-450. Benoxaprofen exhibits significant toxicity: it not only alters cellular redox status, uncouples oxidative phosphorylation and disrupts calcium ion homeostasis, but also causes liver injury through the formation of covalent adducts between its active metabolites and hepatic proteins. Benoxaprofen shows strong phototoxicity under ultraviolet irradiation, and induces erythrocyte lysis, mast cell degranulation and histamine release. Benoxaprofen is widely used in studies of urticaria and related phototoxic mechanisms.

Anti-inflammatory agent 78 (compound L-37) is a potent anti-inflammatory agent. Anti-inflammatory agent 78 has significant potency on PGE2, PGE1, COX-2 and COX-1 inhibition. Anti-inflammatory agent 78 can inhibits NO release in LPS-stimulated RAW 264.7 cell line.

5-LO/mPGES1-IN-1 (Compound 16) is a dual inhibitor of microsomal prostaglandin E2 synthase-1 (mPGES-1) and 5-lipoxygenase (5-LO). IC₅₀ values are 0.3 and 0.4 μM, respectively. 5-LO/mPGES1-IN-1 has anti-inflammatory activity.

(S)-Flurbiprofen-d3 (Esflurbiprofen-d3) is the deuterium labeled (S)-Flurbiprofen. (S)-Flurbiprofen is an active enantiomer of Flurbiprofen, with IC₅₀ values of 0.48 μM and 0.47 μM for COX-1 and COX-2, respectively.

mPGES1-IN-10 (Compound 7d) is a potent microsomal prostaglandin E2 synthase-1 (mPGES-1) inhibitor with an IC₅₀ value of 1.0 μM. mPGES1-IN-10 is promising for research of chronic inflammation-related diseases and malignancies such as colorectal cancer.

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.

Benoxaprofen (Standard) is the analytical standard of Benoxaprofen. This product is intended for research and analytical applications. Benoxaprofen (LRCL 3794) is a nonsteroidal anti-inflammatory agent that blocks the biosynthesis of inflammatory mediators such as leukotrienes and prostaglandins by inhibiting 5-LOX, PGH2 synthase and cytochrome P-450. Benoxaprofen exhibits significant toxicity: it not only alters cellular redox status, uncouples oxidative phosphorylation and disrupts calcium ion homeostasis, but also causes liver injury through the formation of covalent adducts between its active metabolites and hepatic proteins. Benoxaprofen shows strong phototoxicity under ultraviolet irradiation, and induces erythrocyte lysis, mast cell degranulation and histamine release. Benoxaprofen is widely used in studies of urticaria and related phototoxic mechanisms.

Benzydamine (hydrochloride) (Standard) is the analytical standard of Benzydamine (hydrochloride). This product is intended for research and analytical applications. Benzydamine hydrochloride is a prostaglandin synthase inhibitor, anti-inflammatory, and has also been reported to have antibacterial activity.

4-Acetylaminoantipyrine (Standard) is the analytical standard of 4-Acetylaminoantipyrine. This product is intended for research and analytical applications. 4-Acetylaminoantipyrine (4-AA) is a derivative of antipyrine (HY-B0171). 4-Acetylaminoantipyrine acts as a PGE2-dependent blocker and inhibitor of cyclooxygenase (COX). 4-Acetylaminoantipyrine can inhibit Cu/ZnSOD. 4-Acetylaminoantipyrine can spontaneously bind with bovine serum albumin (BSA) and alter its conformation.

Viridicatol (Standard) is the analytical standard of Viridicatol (HY-116474). This product is intended for research and analytical applications. Viridicatol is a quinolone alkaloid with anti-inflammatory, antibacterial, antifungal, osteogenic and chondrogenic activities. Viridicatol reduces the phosphorylation levels of ERK, JNK, p38 and STAT6; inhibits MMP-2, MMP-9, NF-κB signaling pathway and PTP1B; downregulates genes related to mast cell activation; and binds to SHN3 to activate the Wnt/SHN3 signaling pathway. Viridicatol inhibits the expression of pro-inflammatory mediators and cytokines, and promotes osteogenic/chondrogenic differentiation. Viridicatol can be used in studies related to fibrosarcoma, allergy, bacterial infection, fungal infection and osteoporosis.

Zomepirac (McN-2783-21-98 free acid) is an orally active prostaglandin synthetase inhibitor. Zomepirac blocks prostaglandin synthesis and inhibits Collagen (HY-P72147)- or Epinephrine (HY-B0447)-induced platelet aggregation. Zomepirac can be used for the research of postoperative pain and osteoarthritis.

Fagaramide is a compound extracted from Zanthoxylum bungeanum with anti-inflammatory activity. It is effective against carrageenan foot swelling in rats and mediates its anti-inflammatory effect partly by inhibiting prostaglandin synthesis. Its activity is about 1/20 of that of indomethacin.

Cryogenine is an alkaloid originally isolated from H. salicifolia that has anti-inflammatory activity. It inhibits prostaglandin synthetase (IC₅₀=424 μM). Cryogenine (100 mg/kg per day, p.o.) reduces paw edema and the mean arthritic index in a rat model of adjuvant-induced polyarthritis.

LY3023703 is an orally active microsomal prostaglandin E synthase-1 (mPGES-1) inhibitor. LY3023703 inhibits the production of PGE₂. LY3023703 is applicable to research related to inflammatory diseases and osteoarthritis pain.