You are here:Home-Inhibitors & Agonists-Immunology/Inflammation-FLAP

Request The Product List ofFLAP FLAP

Cat. No. Product Name CAS No. Information
PC-35038

BI 665915

1360550-04-4 BI 665915 is a highly potent, selective, orally active 5-lipoxygenase-activating protein (FLAP) inhibitor with binding IC50 of 1.7 nM; displays no activity against other enzymes and receptors in the leukotriene pathway such as 5-LO, COX-1 and -2, phospholipase A2, LTA4 hydrolase, BLT1, and BLT2 (IC50s>10 uM); shows functional inhibition of LTB4 production in human whole blood (IC50=45 nM); demonstrates a dose-dependent DMPK relationship and inhibition of LTB4 production in vivo.
PC-35037

ABT-080

189498-57-5 ABT-080 is a potent FLAP inhibitor that inhibits ionophore-stimulated LTB(4) formation with with IC50 of 20 nM; selectively inhibits zymosan-stimulated mouse peritoneal macrophages producing LTC(4) with IC50 of 0.16 nM, 9000-fold selectivity over PGE(2) producing; demonstrates leukotriene inhibition with oral dosing in a rat pleural inflammation model.

Asthma

Discontinued

PC-61975

AZD-5718

AZD-5718 is an orally available small molecule, 5-lipoxygenase activating protein (FLAP) inhibitor.

Heart Failure

Phase 2 Clinical

PC-42116

MK-0591

136668-42-3 A potent, specific and orally active 5-Lipoxygenase-activating protein (FLAP) inhibitor with IC50 of 1.6 nM in FLAP binding assay; has no inhibitory effect on 15-lipoxygenase and platelet 12-lipoxygenase and cyclooxygenase in human PMNLs; potently inhibits leukotriene (LT) biosynthesis in intact human and elicited rat PMNLs with IC50 of 3.1 and 6.1 nM, respectively; inhibits excretion of LTE4 in antigen-challenged allergic animal models.

Asthma

Discontinued

PC-44769

GSK2190915 sodium

1196070-26-4 A potent, selective FLAP inhibitor with binding IC50 of 2.6 nM; inhibits LTB4 synthesis following ionophore challenge in human whole blood with IC50 of 76 nM (5 h incubation); shows good selectivity over CYP3A4, 2C9, and 2D6; exhibits excellent preclinical toxicology, pharmacokinetics and oral bioactivity.

Asthma

Phase 2 Clinical

PC-44768

GSK2190915

936350-00-4 A potent, selective FLAP inhibitor with binding IC50 of 2.6 nM; inhibits LTB4 synthesis following ionophore challenge in human whole blood with IC50 of 76 nM (5 h incubation); shows good selectivity over CYP3A4, 2C9, and 2D6; exhibits excellent preclinical toxicology, pharmacokinetics and oral bioactivity.

Asthma

Phase 2 Clinical

PC-45853

MK-591

147030-01-1 A potent, orally active leukotriene biosynthesis inhibitor that acts by inhibiting 5-lipoxygenase activating protein (FLAP) with IC50 of 1.6 nM in a FLAP binding assay; inhibits leukotriene (LT) biosynthesis in intact human and elicited rat PMNLs with IC50 of 3.1 nM and 6.1 nM, respectively; inhibits the systemic generation of peptidoleukotrienes as measured by urinary LTE4 excretion in dogs (ED50=1 mg/kg).

Asthma

Phase 1 Discontinued

Request The Product List

* Indicates a Required FieldYour information is safe with us.

  • *Product List:
  • *Applicant name:
  • *Email address:
  • *Organization name:
  • *Country:
  • Additional Information:
Contact Us sales@probechem.com