Fiboflapon (GSK2190915) is a potent FLAP(5-Lipoxygenase-activating protein) inhibitor with binding IC50 of 2.9 nM.
ALR-6 is an antagonist of the 5-lipoxygenase (5-LOX) activating protein FLAP and has anti-inflammatory activity. ALR-6 potently inhibits 5-LOX product formation (>80%) in pro-inflammatory M1-MDM and has no significant effect on direct inhibition of 5-LOX[1].
(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 drug metabolism and pharmacokinetics (DMPK) profile and a dose-dependent inhibition of LTB4 production[1].
MK591 is a selective and specific 5-Lipoxygenase-activating protein (FLAP) inhibitor.
AM 103 is a potent and selective FLAP inhibitor, with an IC50 value of 4.2 nM.
(S)-Veliflapon ((S)-BAY X 1005; (S)-DG-031) is an orally active inhibitor of leukotriene biosynthesis and 5-lipoxygenase activating protein (FLAP). (S)-Veliflapon inhibits the formation of leukotriene B4 (LTB4) in rat, mouse and human leukocytes with IC50 values of 0.026 µM, 0.039 µM and 0.22 µM respectively. (S)-Veliflapon showes enantioselectivity in human whole blood[1][2][3].
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[1][2][3].
Fiboflapon sodium (GSK2190915 (sodium salt)) is a potent FLAP(5-Lipoxygenase-activating protein) inhibitor with binding IC50 of 2.9 nM.
FEN1-IN-6 (compound 9) is a potent inhibitor of Flap endonuclease-1 (FEN1, IC50=10 nM), involving in mammalian cells to repair DNA damage. FEN1-IN-6 also targets to related endonuclease, xeroderma pigmentosum G (XPG) with an IC50 value of 23 nM[1].
AM679 is a potent and selective FLAP inhibitor with IC50s of 2.2 nM/0.6 nM/154 nM for FLAP binding/hLA/hWB respectively. IC50 value: 2.2 nM/0.6 nM/154 nM(FLAP binding/hLA/hWB) [1]Target: FLAPin vitro: AM679 showed excellent in vitro inhibition against FLAP. AM679 has an excellent hWB IC50 potency of 154 nM. AM679 showed an improved CYP inhibition profile (IC50 3A4 = 16.7 lM, 2C9 = 3.7 lM, 2D6 >30 lM), no time dependent inhibition against CYP3A4 (0.003 min-1 vs 0.057 min-1 for troleandomycin control 10 uM) and no CYP3A4 induction.in vivo: AM679 was profiled in a rodent bronchoalveolar lavage (BAL) model to measure its ability to inhibit production ofleukotrienes in vivo.16 Oral administration of 39 (10 mg/kg as the sodium carboxylate salt) 4 h prior to ionophore challenge reduced LTB4 and CysLT levels in the rodent lung lavage fluid by 98% and 87%, respectively, with corresponding average rodent plasma levels of 605 nM (3 h post dose, rat blood LTB4 IC50 = 125 nM).
ALR-27 is an antagonist of the 5-lipoxygenase (5-LOX) activating protein FLAP and has anti-inflammatory activity. ALR-27 potently inhibits 5-LOX product formation (>80%) in pro-inflammatory M1-MDM, with no significant direct inhibition of 5-LOX. ALR-27 not only reduces prostaglandin and leukotriene (LT) production in neutrophils but also increases the production of specialized prolytic mediators in specific human macrophage phenotypes[1].
MK886 is a 5-lipoxygenase-activating protein inhibitor and a leukotriene biosynthesis inhibitor (IC50=2.5 nM).
FEN1-IN-5 (compound 12A) is a potent inhibitor of Flap endonuclease-1 (FEN1, IC50=12 nM), involving in DNA repair[1].
FEN1-IN-7 (compound 16) is a selective inhibitor of Flap endonuclease-1 (FEN1, IC50=18 nM), involving in mammalian cells to repair DNA damage. FEN1-IN-7 also targets to related endonuclease, xeroderma pigmentosum G (XPG) with an IC50 value of 3.04 μM. FEN1-IN-7 increases the cellular sensitivity of cancer cells to potent DNA alkylating agents or methylating agents[1].
MK591 (free acid) is a selective and specific 5-Lipoxygenase-activating protein (FLAP) inhibitor with an IC50 value of 1.6 nM in a FLAP binding assay.