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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
48 Results for "
mPGES-1
" in MedChemExpress (MCE) Product Catalog:
Products (48)
48 Results for "mPGES-1" in MCE Product Catalog:
3
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Dienogest (STS-557) is an orally active and selective progesterone receptor agonist that effectively reduces the gene expression of COX-2, mPGES-1 and aromatase. Dienogest also inhibits the mRNA and protein expression of PGE2 synthase and the activation of NF-κB. Dienogest can be used in studies of endometriosis, menopause and menorrhagia [1] .
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2 Cited Publications
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CAY10526 is an inhibitor of Y-box binding protein 1 (YB-1) and microsomal prostaglandin E2 synthase 1 (mPGES1). CAY10526 inhibits the production of PGE2 by suppressing YB-1 and mPGES1. CAY10526 induces cell apoptosis (apoptosis) and inhibits the JAK/STAT, TGF-β/Smad3 and PI3K/AKT signaling pathways. CAY10526 can be used in research related to melanoma, prostate cancer, esophageal adenocarcinoma, T-cell lymphoma, etc [1] .
1
1 Cited Publications
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MF63 is a selective and orally active inhibitor of mPGES-1. MF63 reduces the accumulation of PGE2, relieves pyresis, hyperalgesia, and inflammatory pain by inhibiting mPGES-1 [1].
Synonyms: BI 1029539; GS-248; OX-MPI
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Vipoglanstat (BI 1029539), a carboxamide, is a potent and selective, non-peptide and orally active small molecular inhibitor of human prostaglandin E synthase 1 (mPGES-1). Vipoglanstat also has anti-inflammatory activity [1] .
Cat. No.: HY-W749694
CAS No.: 76735-58-5
Synonyms: Canniflavone
Category:
Synonyms: ISC-27864; GRC-27864
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Zaloglanstat (ISC-27864; GRC-27864) is a selective, orally active microsomal mPGES-1 inhibitor. Zaloglanstat has an IC50 of 5 nM for human mPGES-1 without significant inhibitory effect on COX-1/2 (IC50 >10 μM). Zaloglanstat blocks the conversion of arachidonic acid metabolite prostaglandin PGH2 to prostaglandin PGE2, thereby inhibiting inflammation-related PGE2 overproduction and reducing inflammatory responses and pain. Zaloglanstat inhibits IL-1β-induced PGE2 release in A549 cells and human synovial fibroblasts in vitro. Zaloglanstat inhibits PGE2 release in pig and dog whole blood with IC50s of 161 nM and 154 nM, respectively. Zaloglanstat can be used in the study of asthma, osteoarthritis, and neurodegenerative diseases [1] .
Synonyms: AAD-2004
Target:
Prostaglandin Receptor Free Radical Scavengers PGE synthase Reactive Oxygen Species (ROS) Apoptosis
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Crisdesalazine (AAD-2004) is a microsomal prostaglandin E2 synthase-1 (mPGES-1) inhibitor. Crisdesalazine acts as a potent free radical scavenger that directly neutralizes reactive oxygen species (ROS) including hydrogen peroxide, exerting neuroprotective effects against apoptosis and axonal damage. Crisdesalazine inhibits PGE2 production, mediates inflammatory responses, and promotes the conversion of macrophages from the pro-inflammatory M1 phenotype to the anti-inflammatory M2 phenotype. Crisdesalazine is applicable to neuroprotection research in multiple sclerosis and spinal cord injury [1] .
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4-CPPC is a selective MIF-2 inhibitor with a Ki of 33 µM. 4-CPPC inhibits the COX2/PGE2 pathway, reduces the levels of COX2 and mPGES-1, and decreases the production of PGE2. 4-CPPC attenuates the formation of early atherosclerotic lesions in hyperlipidemic mice, and lowers the levels of circulating inflammatory cytokines and chemokines. 4-CPPC inhibits MIF-2-triggered cell migration. 4-CPPC improves hindlimb motor function in rats with contusion-induced spinal cord injury. 4-CPPC can be used in studies related to atherosclerosis and spinal cord injury [1] .
Cat. No.: HY-19622
CAS No.: 1221971-47-6
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PF-9184 is a potent and highly selective inhibitor of human microsomal prostaglandin E synthase-1 (mPGES-1), with an IC50 of 16.5 nM. PF-9184 inhibits IL-1β-induced PGE2 synthesis in vitro [1].
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mPGES-1-IN-2 (compound III) is a benzimidazole-based mPGES-1 inhibitor that also inhibits adipophysin PGD synthase (I-PGDS) (5 μM, IR=60 %). mPGES-1-IN-2 reduces PGE2 production and tends to reduce levels of other prostaglandins. mPGES-1-IN-2 effectively inhibits acute inflammation in an air sac model stimulated by Carrageenan (HY-125474) in mice [1].
Cat. No.: HY-162387
CAS No.: 2171000-87-4
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UK4b is a highly selective microsomal prostaglandin E2 synthase-1 (mPGES-1) inhibitor. UK4b possesses anti-inflammatory and analgesic effects. UK4b can block the growth of abdominal aortic aneurysms in mice [1].
Cat. No.: HY-149202
Purity: 99.62%
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UT-11 is a potent and blood-brain barrier-permeable microsomal prostaglandin E synthase-1 (mPGES-1) inhibitor with IC50s of 0.10 μM and 2.00 μM for inhibiting PGE2 production in human (SK-N-AS) and murine (BV2) cells, respectively [1].
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YS121 is a dual inhibitor of microsomal prostaglandin E2 synthase-1 (mPGES-1; IC50 = 3.4 μM) and 5-lipoxygenase (5-LOX; IC50 = 6.5 μM). YS121 exhibits direct, reversible, and specific binding to mPGES-1 (KD = 10-14 μM) [1]. YS121 dose-dependently reduces PGE2 production with an EC50 of 12 μM in IL-1β-stimulated A549 cells . YS121 (compound 9) activates PPAR-α and -γ (EC50 = 1 and 3.6 μM, respectively) . YS121 exhibits anti-inflammatory efficiency in human whole blood as well as in vivo. YS121 can be used for pleurisy research [1].
Cat. No.: HY-178505
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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 [1].
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PF-4693627 is a potent, selective and orally bioavailable microsomal prostaglandin E synthase-1 (mPGES-1) inhibitor (IC50=3 nM) for the treatment of inflammation caused by osteoarthritis (OA) and rheumatoid arthritis (RA) [1].
Cat. No.: HY-178794
CAS No.: 3038861-75-2
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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 [1].
Cat. No.: HY-156612
CAS No.: 1422203-86-8
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Friluglanstat is a prostaglandin E synthase (mPGES-1) inhibitor, with anti-inflammatory activity [1].
Cat. No.: HY-169430
CAS No.: 3038861-74-1
Target:
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 [1].
Cat. No.: HY-179041
CAS No.: 924851-91-2
Target:
PGE synthase Prostaglandin Receptor MDM-2/p53 Amino acid Transporter Glutathione Peroxidase Ferroptosis
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SZ0232 is a selective mPGES-2 inhibitor. SZ0232 binds to the active site of mPGES-2 via hydrogen bonds and π-π stacking, reduces the production of prostaglandin E2 (PGE2) and blocks the PGE2-EP3 pathway. SZ0232 regulates Ferroptosis by activating the heme-dependent p53/SLC7A11/GPX4 axis, inhibits lipid peroxidation, and protects renal tubules. SZ0232 enhances glucose-stimulated insulin secretion, inhibits β-cell senescence, and improves glucose homeostasis. SZ0232 reduces renal lipid accumulation, alleviates fibrosis, and ameliorates renal dysfunction in diabetic mice. SZ0232 inhibits renal cyst growth in polycystic kidney disease models. SZ0232 exhibits an insulinotropic effect that strengthens with the increase of animal age. SZ0232 can be used in studies related to type 2 diabetes, acute kidney injury, diabetic kidney disease, and autosomal dominant polycystic kidney disease [1] .
Cat. No.: HY-100864
CAS No.: 1469976-70-2
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mPGES1-IN-3 (Compound 17d) is a potent and selective microsomal prostaglandin E2 synthase-1 (mPGES-1) inhibitor, which exhibits excellent mPGES-1 enzyme (IC50: 8 nM), cell (A549 IC50: 16.24 nM) and human whole blood potency (IC50: 249.9 nM) [1].
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
