| Cat. No. |
Product Name |
CAS No. |
Information |
| H9180 |
Diflapolin
|
724453-98-9 |
Diflapolin is a highly active dual 5-lipoxygenase-activating protein (FLAP)/soluble epoxide hydrolase (sEH) inhibitor with marked anti-inflammatory efficacy and high target selectivity; Diflapolin inhibits 5-LOX product formation in intact human monocytes and neutrophils with IC50s of 30 and 170 nM, respectively, and suppressed the activity of isolated sEH (IC50=20 nM). |
| H3988 |
Quiflapon sodium
|
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). |
| H3987 |
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. |
| H3986 |
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. |
| H3985 |
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. |
| H3984 |
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. |
| H3983 |
AZD5718
|
2041075-86-7 |
AZD5718 (Atuliflapon,AZD-5718, AZD 5718) is a novel potent 5-lipoxygenase activating protein (FLAP) inhibitor with binding IC50 of 6.3 nM; exhibits LTB4 inhibition in human whole blood assays with IC50 of 39 nM; reduce the production of pro-inflammatory and vasoactive leukotrienes both in vitro and in vivo. |
| H3981 |
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. |
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