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HPGDS inhibitor
HPGDS inhibitor 1 is a novel and selective Hematopoietic Prostaglandin D Synthase (HPGDS) inhibitor with an IC50 Value of 0.7 nM.- Beixian Zhou, .et al. , Chin Med, 2023, Oct 27;18(1):139 PMID: 37891648
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mPGES-1 Inhibitor
Zaloglanstat is a selective microsomal prostaglandin E synthase-1 (mPGES-1) inhibitor, demonstrating an IC50 of 5 nM for human mPGES-1 while sparing COX-1 and COX-2 with IC50 values greater than 10 μM. It effectively inhibits the conversion of prostaglandin PGH2 to prostaglandin PGE2, thereby mitigating inflammation-related overproduction of PGE2 and alleviating pain. In vitro studies show that Zaloglanstat reduces IL-1β-induced PGE2 release in A549 cells and human synovial fibroblasts. It is applicable in research exploring asthma, osteoarthritis, and neurodegenerative diseases, and exhibits effective inhibition of PGE2 release in whole blood from pig and dog models with IC50 values of 161 nM and 154 nM, respectively. -
mPGES-1 Inhibitor
Crisdesalazine is a selective inhibitor of microsomal prostaglandin E2 synthase-1 (mPGES-1). It demonstrates significant biological activity as a free radical scavenger, effectively neutralizing reactive oxygen species (ROS) such as hydrogen peroxide, thereby providing neuroprotective benefits against apoptosis and axonal damage. By inhibiting PGE2 production, Crisdesalazine also modulates inflammatory responses and facilitates the conversion of macrophages from the pro-inflammatory M1 to the anti-inflammatory M2 phenotype. This compound is particularly valuable for research focused on neuroprotection in conditions such as multiple sclerosis and spinal cord injury. -
NO/PGE2 Inhibitor
Epibetulinic acid is an inhibitor of nitric oxide (NO) and prostaglandin E2 (PGE2) production. It demonstrates significant anti-inflammatory activity, exhibiting IC50 values of 0.7 μM for NO and 0.6 μM for PGE2 in mouse macrophages (RAW 264.7) stimulated with bacterial endotoxin. This compound is valuable for research applications focused on inflammation and immune response modulation. -
PGE2 Antagonist
SC-19220 is a competitive antagonist of the prostaglandin E2 receptor, demonstrating significant effects on bladder physiology. Research indicates that SC-19220 enhances bladder capacity while decreasing voiding efficiency in urethane-anesthetized rats during slow transvesical filling. Additionally, SC-19220 has been shown to restore the balance of granulocyte and monocyte production in bone marrow following burn sepsis, making it a valuable tool for investigations related to inflammatory responses and urinary tract function. -
5-LO/PGE2 Inhibitor
Canniprene is a potent inhibitor of 5-lipoxygenase (5-LO) and cyclooxygenase/microsomal prostaglandin E2 synthase (PGE2), with IC50 values of 0.4 μM and 10 μM, respectively. Derived from Cannabis sativa, Canniprene modifies the biosynthesis of inflammatory eicosanoids and prostaglandins, making it a valuable tool for researching inflammation and related pathways. Its unique mechanism of action positions Canniprene as a potential candidate for studying inflammatory diseases and therapeutic interventions targeting lipid mediators. -
PGE2 Inhibitor
Saikogenin D is an effective PGE2 inhibitor isolated from Bupleurum chinense. This compound exhibits significant anti-inflammatory properties by activating epoxygenases, leading to the conversion of arachidonic acid into epoxyeicosanoids and dihydroxyeicosatrienoic acids, which subsequently suppress PGE2 production. Saikogenin D also induces an increase in intracellular calcium levels ([Ca2+]i) through the release of Ca2+ from intracellular stores, making it a valuable tool for studying inflammatory pathways. -
PGE1 Analogue
SC 34301, an orally active PGE1 analogue, exhibits potent anti-inflammatory properties. It has been shown to significantly reduce bacterial translocation and enhance survival rates in burned mouse models. This compound is valuable for research applications focusing on inflammation, tissue repair, and the physiological effects of prostaglandin analogues. -
PGE2 Analog
Prostaglandin E2 Ethanolamide (PGE2-EA) is a biologically active analog of Prostaglandin E2, chiefly targeting the modulation of inflammatory responses. It is formed enzymatically through the COX-2-mediated oxygenation of endocannabinoids. PGE2-EA demonstrates the ability to influence the production of the pro-inflammatory cytokine TNF-α in human blood and monocytic cells, making it a valuable tool for research in inflammation and immunology. -
PGE2 Inhibitor
(+)-Oxypeucedanin methanolate is a potent inhibitor of prostaglandin E2 (PGE2) synthesis. This natural compound exhibits significant anti-inflammatory properties, making it a valuable reagent in studies focused on inflammation and pain modulation. Research applications include investigating the pathways of prostaglandin synthesis and exploring potential therapeutic interventions for inflammatory diseases. -
PGE2 Enantiomer
ent-Prostaglandin E2 (ent-PGE2) is an enantiomer of Prostaglandin E2 that serves as a poor substrate for 15-hydroxyprostaglandin dehydrogenase. This differential substrate activity can be leveraged in various biochemical studies to investigate the enzymatic pathways and regulatory mechanisms involving prostaglandins. Research applications include studying the physiological effects of PGE2 and the role of its enantiomers in inflammatory processes and cell signaling pathways. -
PGE1/PGE2 Metabolite
Tetranor-Prostaglandin E1 is a metabolite of Prostaglandin E1, resulting from β-oxidation processes. This compound serves as a crucial biomarker in studies related to prostaglandin metabolism and pathways. It is commonly utilized in research involving inflammatory responses and various physiological processes mediated by prostaglandins. -
PGE2 Precursor
Prostaglandin E2 isopropyl ester serves as a precursor for Prostaglandin E2 (PGE2). This compound is instrumental in various biological processes, including inflammation and modulation of immune responses. Researchers commonly utilize it in studies focused on prostaglandin synthesis and signaling pathways related to pain, edema, and cellular growth. Its role in mediating physiological functions makes it a valuable reagent for elucidating mechanisms in both basic and applied biomedical research. -
PGE2 Antagonist
SC-42867 is a potent PGE2 antagonist, specifically designed to inhibit prostaglandin E2 signaling pathways. This compound is metabolized in the liver through mechanisms such as oxidative N-dealkylation and aromatic hydroxylation. SC-42867 is highly relevant for studies focused on metabolic conditions, allowing researchers to explore the biochemical implications of PGE2 modulation in various physiological processes. -
PGE2 Analogue
FCE 20700 is an orally active analogue of prostaglandin E2 (PGE2) that primarily targets gastric mucosal integrity. It demonstrates the ability to prevent gastric mucosal damage and inhibit both gastric acid and pepsin secretion. This compound is valuable for research into gastrointestinal ulcers and related disorders, providing insights into therapeutic strategies for gastrointestinal protection. -
NO/PGE2 Inhibitor
Salviifoside A is a phenolic glycoside that acts as an inhibitor of nitric oxide (NO) and prostaglandin E2 (PGE2) production. Isolated from the leaves of Alangium salviifolium, Salviifoside A effectively suppresses LPS-induced nitric oxide and prostaglandin E2 production in macrophages while maintaining cell viability. This compound is valuable for research focused on inflammatory responses and the modulation of macrophage activation. -
PGE2 Metabolite
13,14-Dihydro-15-keto-tetranor prostaglandin E2 is a novel metabolite of Prostaglandin E2, functioning primarily as a bioactive mediator in various physiological processes. As a key derivative, it is involved in studies exploring the metabolic pathways of prostaglandins and their implications in inflammation and other biological responses. This compound has significant applications in research focused on prostaglandin signaling and its role in disease mechanisms. -
PGE2 Analog
8-Iso-16-cyclohexyl-tetranor prostaglandin E2 is a PGE2 analog that exhibits potent biological activity by modulating various physiological processes. It engages the prostaglandin receptors, influencing pathways related to inflammation, pain, and vascular regulation. This compound is valuable for research applications focused on the roles of prostaglandins in disease models, as well as studies investigating receptor-targeted therapies. -
PGE1 Analog
15-Methylprostaglandin E1 is an analog of prostaglandin E1 (PGE1) that primarily targets prostaglandin receptors to elicit cardiovascular effects. It demonstrates a positive chronotropic effect, leading to increased heart rate and enhanced levels of nicardipine. This compound is widely utilized in studies related to circulatory system regulation and pharmacological investigations into heart rate modulation. -
PGE2 Analog
(15S)-15-Methylprostaglandin E2 is a synthetic analog of prostaglandin E2 that primarily targets the PGE2 receptor. This compound exhibits significant biological activity by promoting cytoprotection in gastrointestinal cells and may inhibit gastrointestinal bleeding. Its applications in research include studies on inflammation, gastrointestinal health, and the pharmacological roles of prostaglandins in various biological processes. -
PGE2 Inducer
5S(6R)-EET is a metabolite derived from arachidonic acid that acts as a potent inducer of prostaglandin E2 (PGE2) synthesis. This compound enhances intracellular calcium levels and inhibits sodium absorption, contributing to membrane depolarization. Its biological activity makes it a valuable tool for research focused on the regulatory roles of prostaglandins in various physiological processes. -
PGE2 Analog
16-Phenoxy tetranor Prostaglandin E2 is an analog of prostaglandin E2 (PGE2) that serves as a potent modulator of various biological processes. This compound exhibits significant biological activity by influencing the prostaglandin pathway, making it valuable for studying inflammatory responses and reproductive biology. Additionally, its role as a minor metabolite of sulprostone in human plasma provides insights into pharmacokinetics and metabolic pathways relevant to drug development and therapeutic applications. -
COX-2/PGE2 Inducer
Rebamipide-d4 is a deuterium-labeled derivative of Rebamipide, primarily targeting cyclooxygenase-2 (COX-2). This compound induces COX-2 expression and elevates prostaglandin E2 (PGE2) levels, thereby enhancing gastric mucosal defense mechanisms in a COX-2-dependent manner. Rebamipide-d4 is utilized in various research applications focused on gastric protection and the modulation of inflammatory responses. -
PGE2 Inducer
5R(6S)-EET is a metabolite derived from arachidonic acid that functions as a PGE2 inducer. It activates the synthesis of endogenous prostaglandin E2, leading to inhibition of sodium absorption, an increase in intracellular calcium levels, and enhanced depolarization of transmembrane voltage. This compound displays stereoselectivity, exhibiting differential activity compared to its stereoisomer, 5S(6R)-EET. Its biological effects make it a valuable tool for研究 applications focusing on prostaglandin signaling and related pathways. -
PGE1 Prodrug
Ecraprost is a prodrug of prostaglandin E1, designed to enhance the bioavailability of PGE1 in therapeutic applications. It effectively inhibits platelet adhesion and macrophage infiltration, as well as the expression of proliferating cell nuclear antigen in injured arterial walls. Ecraprost is utilized in research related to cardiovascular health and vascular injury repair. -
PGE1 Metabolite
13,14-Dihydro-15-keto-PGE1 is a metabolite of prostaglandin E1 (PGE1) that exhibits inhibitory effects on platelet aggregation. It has been shown to inhibit ADP-induced aggregation in human isolated platelet-rich plasma with an IC50 value of 14.8 μg/mL. This compound is useful in research applications focusing on thrombotic disorders and the role of prostaglandins in platelet function. -
NO/mPGES-1 Inhibitor
Shanciol B is a selective inhibitor of nitric oxide (NO) production and microsomal prostaglandin E synthase-1 (mPGES-1). Isolated from the ethyl acetate extract of Pholidota imbricate, Shanciol B exhibits notable anti-inflammatory properties and demonstrates effective 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging activity. This compound is valuable for research applications focused on inflammation and oxidative stress. -
mPGES1 Inhibitor
CAY10526 is a selective inhibitor of microsomal prostaglandin E2 synthase-1 (mPGES1), exerting its effects by specifically modulating mPGES1 expression without influencing cyclooxygenase-2 (COX-2). This compound effectively reduces PGE2 production, leading to significant suppression of tumor growth and enhanced apoptosis in melanoma xenografts. CAY10526 downregulates anti-apoptotic proteins BCL-2 and BCL-XL while elevating levels of pro-apoptotic proteins BAX and BAK, along with cleaved caspase-3, promoting cell death. It demonstrates potent cytotoxicity with an IC50 of less than 5 μM in melanoma cell lines expressing mPGES1, making it valuable for cancer research and therapeutic studies. -
mPGES-1 Inhibitor
Vipoglanstat is a potent and selective non-peptide inhibitor of human microsomal prostaglandin E synthase-1 (mPGES-1). As a carboxamide derivative, it demonstrates significant anti-inflammatory activity, making it a valuable tool in research focusing on inflammation-related diseases. Its oral bioavailability facilitates in vivo studies aimed at understanding the role of mPGES-1 in various pathological conditions. -
PGE synthase Inhibitor
Zomepirac sodium salt is a potent inhibitor of prostaglandin E synthase, exhibiting significant anti-inflammatory properties. As a non-steroidal anti-inflammatory drug (NSAID), Zomepirac sodium salt is primarily utilized in research to study prostaglandin biosynthesis and related inflammatory processes. It is noteworthy that this compound has been associated with immune-mediated liver injury, highlighting its importance in pharmacological safety assessments. -
mPGES-1 Inhibitor
mPGES1-IN-7 is a benzimidazole-derived inhibitor targeting microsomal prostaglandin E synthase-1 (mPGES-1). It significantly reduces prostaglandin E2 (PGE2) production and exhibits inhibitory effects on other prostaglandins. mPGES1-IN-7 has demonstrated effectiveness in mitigating acute inflammation, as evidenced in a Carrageenan-induced air sac model in mice, making it a valuable tool for research in inflammation and related biological pathways. -
mPGES-1 Inhibitor
UK4b is a selective inhibitor of microsomal prostaglandin E2 synthase-1 (mPGES-1). This compound exhibits anti-inflammatory and analgesic properties, making it a valuable tool for research on pain and inflammation. Additionally, UK4b has demonstrated the ability to inhibit the growth of abdominal aortic aneurysms in murine models, highlighting its potential applications in cardiovascular research. -
mPGES-1 Inhibitor
PF-4693627 is a potent and selective inhibitor of microsomal prostaglandin E synthase-1 (mPGES-1) with an IC50 of 3 nM. This compound exhibits oral bioavailability and is designed for research into inflammatory conditions, particularly those related to osteoarthritis and rheumatoid arthritis. Its ability to inhibit mPGES-1 makes it a valuable tool for investigating pathways involved in inflammation. -
mPGES-1 Inhibitor
PF-9184 is a potent and highly selective inhibitor of human microsomal prostaglandin E synthase-1 (mPGES-1), exhibiting an IC50 of 16.5 nM. It effectively inhibits IL-1β-induced prostaglandin E2 (PGE2) synthesis in vitro, making it a valuable tool for studying inflammatory processes. This compound is applicable in research focused on pain, inflammation, and other related pathways. -
mPGES-1 Inhibitor
CAY10589 is a selective inhibitor of the enzyme mPGES-1, which plays a critical role in inflammatory responses. This compound is primarily utilized in research to study the mechanisms of inflammation and its associated pathways. Importantly, CAY10589 does not significantly influence the differentiation of bone marrow myeloid precursor cells into M2-like tumor-associated macrophages (TAMs), making it a valuable tool for dissecting inflammatory processes without altering macrophage polarization. -
mPGES1 Inhibitor
mPGES1-IN-9 is a selective inhibitor of the microsomal prostaglandin E synthase-1 (mPGES1) enzyme, exhibiting an IC50 value of 0.5 μM. This compound is utilized in anti-inflammatory research, facilitating studies aimed at understanding the role of mPGES1 in various inflammatory processes. Its effective inhibition makes it a valuable tool for investigating potential therapeutic strategies in inflammatory diseases. -
PGE synthase Inhibitor
mPGES1-IN-4 is a potent inhibitor of microsomal prostaglandin E synthase-1 (mPGES-1), effectively reducing PGE2 production at submicromolar concentrations. This compound demonstrates notable anti-inflammatory activity, particularly in in vivo models of acute inflammation, by selectively targeting the mPGES-1 pathway. Its application in research includes investigating the role of PGE2 in inflammatory processes and potential therapeutic interventions. -
PGE2 Inhibitior
(+)–ε-Viniferin is a stilbene compound that acts as a PGE2 inhibitor, demonstrating significant anti-inflammatory properties. This compound is orally active and has been shown to reduce fat accumulation, making it a valuable tool for research focused on inflammation and obesity. -
mPGES-1 Inhibitor
AF3442 is a selective inhibitor of mPGES-1, exhibiting an IC50 value of 0.06 μM. This compound effectively reduces PGE2 generation from monocytes, even in the presence of plasma proteins, demonstrating its practical application in biological systems. AF3442's selectivity for mPGES-1 over other prostanoids such as TXB2, PGF2α, and 6-keto-PGF1α supports its use in research focused on analgesia and inflammation pathways. -
PGE Inhibitor
mPGES1-IN-6 is a potent inhibitor of microsomal prostaglandin E synthase-1 (mPGES-1) with an IC50 value of 0.03 μM. By effectively blocking mPGES-1, this compound plays a crucial role in reducing prostaglandin E2 synthesis, making it valuable for studies related to inflammation and pain modulation. mPGES1-IN-6 is suitable for research applications focused on anti-inflammatory drug discovery and the investigation of related signaling pathways. -
PGE2 Synthase Inhibitor
5-trans U-44069 is a selective inhibitor of prostaglandin E2 synthase, effectively modulating the synthesis of this key inflammatory mediator. Its primary mechanism of action involves the blockade of prostaglandin E2 formation, making it a valuable tool for investigating the role of PGE2 in various biological processes. This compound is suitable for research applications related to inflammation, pain, and cardiovascular studies. -
PGE synthase Inhibitor
Friluglanstat is a selective inhibitor of microsomal prostaglandin E synthase-1 (mPGES-1), targeting the synthesis of prostaglandin E2. This compound exhibits anti-inflammatory activity by reducing prostaglandin levels, making it a valuable tool for investigating inflammatory pathways. It is applicable in research focused on inflammation, pain relief, and related diseases. -
mPGES-1Inhibitor
AGU661 is a potent inhibitor of Microsomal Prostaglandin E2 Synthase 1 (mPGES-1) with an IC50 of 0.22 nM. It effectively reduces PGE2 production in human pro-inflammatory M1 macrophages and activated monocytes, while sparing other lipid mediator pathways. Although AGU661 exhibits poor metabolic stability and high plasma protein binding, its incorporation into PLGA-based nanoparticles significantly enhances its bioactivity. This compound is suited for research related to inflammatory disorders. -
PGE synthase Inhibitor
mPGES1-IN-5 is a polysubstituted pyrimidine compound that serves as a selective inhibitor of microsomal prostaglandin E synthase-1 (mPGES-1). This compound demonstrates potent submicromolar inhibition of PGE2 production, primarily exerting its anti-inflammatory effects through mPGES-1 blockade. It is particularly useful in research related to inflammation and can be applied in various acute inflammation models in vivo to study its therapeutic potential. -
PGE Inhibitor
BRP-201 is a selective inhibitor of microsomal prostaglandin E synthase-1 (mPGES-1), demonstrating an IC50 value of 0.42 μM. This compound exhibits potent anti-inflammatory properties, making it a valuable tool for research in inflammatory diseases. Its specificity for mPGES-1 supports its potential application in the development of next-generation anti-inflammatory therapeutics. -
5-LO/mPGES-1 Inhibitor
5-LO/mPGES1-IN-1 is a dual inhibitor of 5-lipoxygenase (5-LO) and microsomal prostaglandin E2 synthase-1 (mPGES-1), exhibiting IC50 values of 0.3 μM and 0.4 μM, respectively. This compound demonstrates significant anti-inflammatory activity, making it a valuable tool for research in inflammatory pathways. Applications include studies focused on the modulation of inflammatory responses, providing insights into potential therapeutic strategies for related diseases. -
mPGES-1 Inhibitor
AGU654 is a selective mPGES-1 inhibitor with an IC50 of 2.9 nM, acting primarily on the microsomal prostaglandin E synthase-1 (mPGES-1) enzyme. By inhibiting this enzyme, AGU654 disrupts the conversion of arachidonic acid to prostaglandin E2 (PGE2), thereby reducing inflammatory responses, pain, and fever. In cellular models, AGU654 effectively suppresses PGE2 production in response to bacterial exotoxins while maintaining the synthesis of other prostaglandins. Furthermore, in guinea pig models, it demonstrates significant anti-inflammatory, analgesic, and antipyretic properties, highlighting its potential for research in inflammatory diseases and pain management. -
PGE synthase Inhibitor
Fagaramide is a potent inhibitor of prostaglandin E synthase, demonstrating significant anti-inflammatory properties. Extracted from Zanthoxylum bungeanum, it effectively reduces carrageenan-induced foot swelling in rat models. This compound serves as a valuable tool for research into inflammation mechanisms and potential therapeutic applications targeting prostaglandin synthesis. Its biological activity is approximately 1/20 that of indomethacin, making it a noteworthy candidate for further exploration in inflammatory studies. -
PGE synthase Inhibitor
Cryogenine is an alkaloid that functions as a selective inhibitor of prostaglandin E synthase, exhibiting significant anti-inflammatory properties. With an IC50 value of 424 μM, Cryogenine effectively attenuates inflammatory responses. In experimental models, administration at doses of 100 mg/kg per day has shown a reduction in paw edema and a decreased mean arthritic index in rats with adjuvant-induced polyarthritis. This makes Cryogenine a valuable reagent for researching inflammation and related disorders. -
Pge Synthase Inhibitor
5-trans U-46619 is an inhibitor of prostaglandin E synthase, which plays a critical role in the biosynthesis of prostaglandins. At a concentration of 10 μM, 5-trans U-46619 demonstrates an inhibition of less than 20% on PGE synthase activity. This compound is suitable for research applications investigating the modulation of inflammatory pathways and the role of prostaglandins in various biological processes.

