PGE Synthase

PGE synthase inhibitors act on the terminal enzymes that convert prostaglandin H2 into prostaglandin E2. Microsomal prostaglandin E (PGE) synthase-1 (mPGES-1) was described in 1999 as a glutathione-dependent enzyme induced by inflammatory stimuli. Inhibitors of this enzyme reduce prostaglandin E2 formation without blocking the upstream cyclooxygenases. MF63 and mPGES1-IN-3 are mPGES-1 inhibitors for inflammation and pain research. The list also covers the prostaglandin D synthases, which turn the same precursor into prostaglandin D2. Hematopoietic prostaglandin D synthase (H-PGDS) was cloned and its crystal structure solved in 1997. HPGDS inhibitor 1 and hPGDS-IN-1 target H-PGDS, whereas AT 56 inhibits lipocalin-type prostaglandin D synthase (L-PGDS).

3 Items

  • EP4 receptor antagonist 7
    Cat. No.
    A35920

    EP4 receptor antagonist 7

    EP4 receptor antagonist 7 is a selective antagonist of the prostaglandin E2 (PGE2) receptor subtype EP4, demonstrating an IC50 value of 1.1 nM. This compound effectively inhibits PGE2-induced β-arrestin recruitment in HEK293 cells with an IC50 of 0.9 nM and downregulates the expression of several important mRNAs, including IL-4 and Arg1, in RAW 264.7 macrophages. Additionally, EP4 receptor antagonist 7 shows potential in combination with anti-PD-1 antibodies to inhibit tumor growth and enhance CD8+ T cell infiltration in a CT26 murine colon cancer model, making it a valuable tool for cancer immunotherapy research.

    1 mg
    $195.00
    5 mg
    $600.00
    All 3 sizes
  • SC-19220
    Cat. No.
    A63059

    SC-19220

    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.

    1 mg
    $30.00
    5 mg
    $75.00
    All 7 sizes
  • SC-42867
    Cat. No.
    A63240

    SC-42867

    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.

    25 mg
    $1,275.00
    50 mg
    $1,625.00
    All 3 sizes

3 Items

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