FLAP Inhibitor

AM 103 is a potent and selective FLAP inhibitor, with an IC₅₀ value of 4.2 nM.

(S)-BI 665915 is an orally active oxadiazole-containing 5-lipoxygenase-activating protein (FLAP) inhibitor with an IC₅₀ of 1.7 nM for FLAP binding. (S)-BI 665915 inhibits FLAP functional in human whole blood with an IC₅₀ of 45 nM. (S)-BI 665915 demonstrates an excellent cross-species agent metabolism and pharmacokinetics (DMPK) profile and a dose-dependent inhibition of LTB₄ production.

MK-886 (L 663536) sodium salt is a potent, cell-permeable and orally active FLAP (IC₅₀ of 30 nM) and leukotriene biosynthesis (IC₅₀s of 3 nM and 1.1 μM in intact leukocytes and human whole blood, respectively) inhibitor. MK-886 sodium salt is also a non-competitive PPARα antagonist and can induce apoptosis.

SC13 is an orally active, selective Flap structure-specific endonuclease 1 (FEN1) inhibitor and mu opioid receptor (MOR) activator. SC13 impairs DNA damage repair and induces apoptosis in cancer cells. SC13 activates cGAS-STING signaling, increases chemokine secretion, and promotes CAR-T cell infiltration at solid tumour sites. SC13 can be used for the research of solid tumours and pain.

BI 665915, a chemical probe, is an orally active and potent 5-lipoxygenase-activating protein (FLAP) inhibitor. BI 665915 inhibits FLAP production that blocks LTB4 biosynthesis in mice. BI 665915 is promising for research of various inflammatory diseases, including respiratory and cardiovascular diseases.

sEH/FLAP-IN-2 is a selective sEH (IC₅₀ = 12.6 nM)/FLAP dual inhibitor. sEH/FLAP-IN-2 highlights the reduction of 5-LOX/FLAP- and sEH-derived LMs, resulting in a favourable redistribution of LMs. sEH/FLAP-IN-2 can be used for the study of peritonitis.

sEH/FLAP-IN-1 (Compound 46A) is a sEH/FLAP inhibitor. sEH/FLAP-IN-1 inhibits 5-LOX product formation in SACM-stimulated PBMCs (EC₅₀: 11 nM). sEH/FLAP-IN-1 inhibit sEH (EC₅₀: 18 nM) and thromboxane production. sEH/FLAP-IN-1 can be used for research of inflammatory diseases.

L-669083 is a leukotriene biosynthesis inhibitor whose structure is based on a mixture of indole and quinoline. In this study, a potent radioiodinated photoaffinity analog of L-689,037, [125I] L-691,678, was developed and characterized for immunoprecipitation studies showing that the quindole series of leukotriene biosynthesis inhibitors directly interact with FLAP. In addition, the results showed that MK-886, L-674,573, and L-689,037 competed with [125I] L-691,678 and [125I] L-669083 for binding to FLAP in a concentration-dependent manner, indicating that these three leukotriene biosynthesis inhibitors share a binding site on FLAP, further demonstrating that FLAP is a suitable target for structurally diverse leukotriene biosynthesis inhibitors.

BRP-7 is a 5-lipoxygenase activating protein (FLAP) inhibitor with an IC₅₀ of 0.31 μM. BRP-7 inhibits the co-localization of 5-lipoxygenase (5-LOX) and FLAP by targeting FLAP, thereby blocking the transfer of arachidonic acid (AA) to 5-LOX and suppressing the production of leukotrienes (LTs) (IC₅₀ = 0.15 μM). BRP-7 does not inhibit cyclooxygenase (COX-1/COX-2) or microsomal prostaglandin E₂ synthase-1 (mPGES-1), and does not affect cell viability or AA release. BRP-7 exhibits significant anti-inflammatory effects in rat pleurisy and mouse peritonitis models. BRP-7 can be used for the study of inflammatory diseases.

ABT-080 is an orally active inhibitor of leukotriene biosynthesis that targets 5-lipoxygenase-activating protein (FLAP). ABT-080 inhibits leukotriene production in intact human neutrophils, mouse peritoneal macrophages and human whole blood, with IC₅₀ values of 20 nM, 0.16 nM and 13 μM, respectively. ABT-080 blocks the leukotriene pathway leading to the synthesis of LTB4 and LTC4, but does not block PGH2 biosynthesis. ABT-080 inhibits leukotriene biosynthesis and bronchoconstriction in mouse models. ABT-080 is used in research related to asthma, pleurisy and allergy.

AZD6642 is a 5-lipoxygenase activating protein (FLAP) inhibitor. AZD6642 can effectively inhibit the production of LTB₄. AZD6642 exhibits high oral bioavailability in rats and dogs. AZD6642 can be used in the research of inflammatory diseases.

Quiflapon (sodium) (Standard) is the analytical standard of Quiflapon (sodium). This product is intended for research and analytical applications. Quiflapon sodium (MK-591 sodium) is a selective and specific 5-Lipoxygenase-activating protein (FLAP) inhibitor. Quiflapon sodium is an orally active Leukotriene biosynthesis inhibitor. Induces apoptosis.

AM103 (free acid) is a selective FLAP inhibitor that can block the first step of the LT pathway, which is 5-LO activation. AM103 (free acid) can inhibit the production of LTB₄ and cysteinyl leukotrienes (CysLT). AM103 (free acid) has anti-inflammatory activity in a mouse model of chronic lung inflammation and can extend the survival time of mice injected with platelet-activating factor. AM103 (free acid) can be used for research on respiratory diseases such as asthma.

Quiflapon (Standard) is the analytical standard of Quiflapon. This product is intended for research and analytical applications. Quiflapon (MK-591) is a selective and specific 5-lipoxygenase-activating protein (FLAP) inhibitor with an IC50?of 1.6 nM in a FLAP binding assay. Quiflapon is also a potent and orally active?Leukotriene biosynthesis (LT)?inhibitor, shows IC50?values of 3.1 and 6.1 nM in intact human and elicited rat PMNLs, respectively. Quiflapon induces cell apoptosis.

ABT-080 free base is an orally active inhibitor of leukotriene biosynthesis that targets 5-lipoxygenase-activating protein (FLAP). ABT-080 free base inhibits leukotriene production in intact human neutrophils, mouse peritoneal macrophages and human whole blood, with IC₅₀ values of 20 nM, 0.16 nM and 13 μM, respectively. ABT-080 free base blocks the leukotriene pathway leading to the synthesis of LTB4 and LTC4, but does not block PGH2 biosynthesis. ABT-080 free base inhibits leukotriene biosynthesis and bronchoconstriction in mouse models. ABT-080 is used in research related to asthma, pleurisy and allergy.

JFD00950 is a human FEN1 inhibitor with an IC₅₀ of 5.5 μM. JFD00950 binds directly to FEN1, alters the secondary structure of this protein, and competitively inhibits its flap cleavage activity by interfering with substrate binding. JFD00950 selectively reduces the viability of cancer cells. JFD00950 can be used in the research of colon cancer and breast cancer.

MK-886 (Standard) is the analytical standard of MK-886. This product is intended for research and analytical applications. MK-886 (L 663536) is a potent, cell-permeable and orally active FLAP (IC50 of 30 nM) and leukotriene biosynthesis (IC50s of 3 nM and 1.1 μM in intact leukocytes and human whole blood, respectively) inhibitor. MK-886 is also a non-competitive PPARα antagonist and can induce apoptosis.

FLAP-IN-1 (Intermediate 14) is a 5-lipoxygenase-activating protein (FLAP) inhibitor with an IC₅₀ value of 654 nM. FLAP-IN-1 can be used in cardiovascular disease research.

FEN1-IN-8 (compund 15) is a selective FEN1 inhibitor, with IC₅₀ values of < 100 nM for FEN1 and 100 nM to 1 μM for EXO1, respectively. FEN1-IN-8 can be used for study of colorectal cancer and gastric cancer.