FLAP-Inhibitors-Modulators-MCE

1、 HYPERLINK https:/www.MedChemE/Targets/FLAP.html FLAP5-lipoxygenase-activating protein; 5-LO activating proteinFLAP (Arachidonate 5-lipoxygenase-activating protein) is an integral membrane protein, which facilitates the transfer of thesubstrate arachidonic acid (AA) to 5-lipoxygenase (5-LO) to produ

2、ce leukotrienes (LTs), and is shown to be indispensable for cellularLT biosynthesis. FLAP transfers arachidonic acid to 5-LOX protein, thereby enabling this enzyme to efficiently produce oxidized lipidproducts (mainly eicosanoids) that are important in cell growth, differentiation and death particul

3、arly apoptosis.www.MedChemE 1 HYPERLINK https:/www.MedChemE/Targets/FLAP.html FLAP HYPERLINK https:/www.MedChemE/Targets/FLAP.html HYPERLINK https:/www.MedChemE/Targets/FLAP.html Inhibitors HYPERLINK https:/www.MedChemE/s-bi-665915.html (S)-BI HYPERLINK https:/www.MedChemE/s-bi-665915.html HYPERLINK

4、 https:/www.MedChemE/s-bi-665915.html 665915 HYPERLINK https:/www.MedChemE/s-bi-665915.html HYPERLINK https:/www.MedChemE/AM_103.html AM103Cat. No.: HY-12995A Cat. No.: HY-14163(S)-BI 665915 is an orally activeoxadiazole-containing 5-lipoxygenase-activatingprotein (FLAP) inhibitor with an IC of 1.7

5、nM50for FLAP binding. (S)-BI 665915 inhibits FLAPfunctional in human whole blood with an IC of 4550nM.AM 103 is a potent and selective FLAP inhibitor,with an IC value of 4.2 nM.50Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1

6、 mg, 5 mg HYPERLINK https:/www.MedChemE/AM679.html AM679Cat. No.: HY-14460 HYPERLINK https:/www.MedChemE/azd5718.html Atuliflapon(AZD5718) Cat. No.: HY-122908AM679 is a potent, selective5-lipoxygenase-activating protein (FLAP) inhibitorwith an IC of 2 nM in a human FLAP membrane50binding assay.Atuli

7、flapon (AZD5718) is an orally activeinhibitor of FLAP (5Lipoxygenase activatingprotein), with an IC of 2 nM. Atuliflapon is used50in the study for coronary artery disease.Purity: 99.72%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 98.14%Clinical Data: Phas

8、e 2Size: 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/diflapolin.html DiflapolinCat. No.: HY-128171 HYPERLINK https:/www.MedChemE/GSK2190915.html Fiboflapon(GSK2190915; AM-803) Cat. No.: HY-15874Diflapolin is a highly active dual5-lipoxygenase-activating protein (FLAP)/solubleepox

9、ide hydrolase (sEH) inhibitor with markedanti-inflammatory efficacy and high targetselectivity.Fiboflapon (GSK2190915; AM-803) is a potent andorally bioavailable 5-lipoxygenase-activatingprotein (FLAP) inhibitor with a potency of 2.9 nMin FLAP binding, an IC of 76 nM for inhibition50of LTB4 in human

10、 blood.Purity: 99.42%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 98.54%Clinical Data: Phase 2Size: 10 mM 1 mL, 5 mg, 10 mg, 50 mg HYPERLINK https:/www.MedChemE/GSK2190915-sodium-salt.html Fiboflapon HYPERLINK https:/www.MedChemE/GSK2190915-sodium-

11、salt.html HYPERLINK https:/www.MedChemE/GSK2190915-sodium-salt.html sodium HYPERLINK https:/www.MedChemE/GSK2190915-sodium-salt.html HYPERLINK https:/www.MedChemE/MK-886.html MK-886(GSK2190915 sodium salt; AM-803 sodium) Cat. No.: HY-15874A (L 663536) Cat. No.: HY-14166Fiboflapon sodium (GSK2190915;

12、 AM-803) is a potentand orally bioavailable 5-lipoxygenase-activatingprotein (FLAP) inhibitor with a potency of 2.9 nMin FLAP binding, an IC of 76 nM for inhibition50of LTB4 in human blood.MK-886 (L 663536) is a potent, cell-permeable andorally active FLAP (IC50 of 30 nM) and leukotrienebiosynthesis

13、 (IC s of 3 nM and 1.1 M in intact50leukocytes and human whole blood, respectively)inhibitor. MK-886 is also a non-competitive PPARantagonist and can induce apoptosis.Purity: 99.91%Clinical Data: Phase 2Size: 10 mM 1 mL, 5 mg, 10 mg, 50 mgPurity: 99.74%Clinical Data: No Development ReportedSize: 10

14、mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/MK-0591.html Quiflapon HYPERLINK https:/www.MedChemE/MK-0591.html HYPERLINK https:/www.MedChemE/MK591.html Quiflapon HYPERLINK https:/www.MedChemE/MK591.html HYPERLINK https:/www.MedChemE/MK591.html sodium(MK-591) Cat. No.: HY-

15、10037 (MK-591 sodium) Cat. No.: HY-50714Quiflapon (MK-591) is a selective and specific5-lipoxygenase-activating protein (FLAP) inhibitorwith an IC of 1.6 nM in a FLAP binding50assay.Quiflapon sodium (MK-591 sodium) is a selectiveand specific 5-Lipoxygenase-activating protein(FLAP) inhibitor. Quiflap

16、on sodium is an orallyactive Leukotriene biosynthesis inhibitor. Inducesapoptosis.Purity: 99.44%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 98.65%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg2 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/veliflapon.html Veliflapon(BAY X 1005; DG-031) Cat. No.: HY-14165