It is known that PGE synthase, also known as prostaglandin E synthase, is made up of a group of at least three structurally and biologically distinct enzymes. PGE synthase converts prostaglandin H2 (PGH2), which is produced by cyclooxygenase (COX), to PGE2. PGES that are associated with membranes include mPGES-1, mPGES-2, and cytosolic PGES (cPGES).
Perinuclear mPGES-1 is a protein that, like COX-2, is markedly upregulated by proinflammatory stimuli and downregulated by anti-inflammatory glucocorticoids. It has a clear functional preference for COX-2 over COX-1. The Golgi membrane-associated protein mPGES-2 is synthesized, and the N-terminal hydrophobic domain is removed by proteolysis to create a mature cytosolic enzyme. This enzyme is functionally coupled with both COX-1 and COX-2 and is expressed rather constitutively in a variety of cells and tissues. cPGES is functionally linked to COX-1 to encourage immediate PGE2 production, and it is constitutively expressed in a wide range of cell types.
| Structure | Cat No. | Product Name | CAS No. | Product Description |
|---|---|---|---|---|
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V74281 | BRP-201 | 2227434-74-2 | BRP-201 is considered a promising research target for next-generation anti-inflammatory drugs to study inflammatory diseases and is a new, potent and specific inhibitor of mPGES-1 with IC50 of 0.42 μM. |
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V74282 | Clopirac | 42779-82-8 | Clopirac is a potent and orally bioactive prostaglandin synthetase inhibitor. |
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V33842 | Dehydroevodiamine hydrochloride | 111664-82-5 | Dehydroevodiamine hydrochloride, the hydrochloride salt of dehydroevodiamine, is a naturally occurring quinazoline alkaloid isolated from the unripe fruit of Evodia rutaecarpa (Rutaceae) with a variety of biological effects such as hypotensive, negative chronotropic, ion channel depressa. |
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V74278 | Friluglanstat | 1422203-86-8 | Friluglanstat is a prostaglandin E synthase (mPGES-1) inhibitor (antagonist) with anti~inflammatory activity. |
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V2882 | HPGDS inhibitor 1 | 1033836-12-2 | HPGDS Inhibitor I (also known as H-PGDS inhibitor 1) is a novel, orally bioavailable, potent and selective inhibitor of Hematopoietic Prostaglandin D Synthase (HPGDS) with IC50 Value of 0.7 nM. |
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V31708 | HPGDS inhibitor 2 | 2101626-26-8 | HPGDS inhibitor 2 (GSK2894631A) is a novel, potent, highly potent and selective hematopoietic prostaglandin D synthase (H-PGDS) inhibitor with an IC50 of 9.9 nM. |
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V4638 | limaprost | 74397-12-9 | Limaprost (formerly ONO1206; OP1206; ONO-1206; OP-1206) is, an alprostadil (prostaglandin E1) analogue, is a novel and potent vasodilator that increases blood flow and inhibits platelet aggregation. |
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V74284 | Limaprost-d3 (Limaprost d3) | 1263190-37-9 | Limaprost-d3 is the deuterium labelled form of Limaprost. |
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V20408 | MF-63 | 892549-43-8 | MF-63 is a novel and selective mPGES-1 inhibitor. |
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V74283 | mPGES-1-IN-1 | 2914158-00-0 | MPGES-1 is considered a promising research target for next-generation anti-inflammatory drugs to study inflammatory diseases, and the IC50 of mPGES-1-IN-1 is 0.03 μM. |
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V14333 | SAR191801 | 1234708-04-3 | SAR191801 (hPGDS-IN-1) is a novel, potent and selecive hPGDS inhibitorwith an IC50 of 12 nM in the Fluorescence Polarization Assay (the EIA assay). |
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V31351 | Sinensetin | 2306-27-6 | Sinensetin is a methylated flavonoid found in fruits that has strong anti-vascular and anti~inflammatory properties. |
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V76382 | UT-11 | UT-11 is a potent, brain-penetrating microsomal prostaglandin E synthetase-1 (mPGES-1) inhibitor that can suppress PGE2 expression in human (SK-N-AS) and mouse (BV2) cells. | |
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V74279 | Zaloglanstat (ISC-27864; GRC-27864) | 1513852-12-4 | Zaloglanstat (ISC-27864) is an inhibitor (blocker/antagonist) of mPGES-1 and may be utilized in research on asthma, osteoarthritis, rheumatoid arthritis, acute or chronic pain, and neurodegenerative diseases. |
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V29803 | Zomepirac sodium salt | 64092-48-4 | Zomepirac sodium salt (McN-2783-21-98) is a potent inhibitor of prostaglandin biosynthesis. |
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