PGE synthase Inhibitor

mPGES1-IN-9 (compound 1_8) is a mPGES1 inhibitor (IC₅₀=0.5 μM), which can be used in anti-inflammatory research.

mPGES1-IN-4 (compound 32) 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.

(+)-ε-Viniferin is a stilbenes compound with PGE2 inhibition effect, and is an orally active anti-inflammatory agent. ε-viniferin is also able to reduce fat accumulation, thus can be used for research of inflammation or obesity.

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.

Antitumor agent-225 is an orally effective and potent HDAC inhibitor with an IC₅₀ value of 4.17 nM. Antitumor agent-225 inhibits HDAC activity by chelating zinc ions through its hydroxamic acid group, downregulates iNOS and COX-2 proteins, and suppresses the production of multiple inflammatory factors induced by LPS (HY-D1056). Antitumor agent-225 can be used for research on cancer and inflammation-related diseases.

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.

Jusneesiinol is a lignan-class prostaglandin synthesis inhibitor and COX-1/COX-2 inhibitor that exerts central analgesic, peripheral analgesic, and antipyretic effects by inhibiting prostaglandin formation, antagonizing prostaglandin receptors, and inhibiting lipid peroxidation. Jusneesiinol can be used in research on pain and fever.

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.