MK-591

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种有效的口服活性白三烯生物合成抑制剂，通过抑制 5-脂氧合酶激活蛋白 (FLAP) 发挥作用，在 FLAP 结合测定中 IC50 为 1.6 nM。

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.

Quiflapon sodium (MK591) and SB203580 are able to block SEB-induced human PBMC cell proliferation. Quiflapon sodium (MK591) down regulates three genes [for cathepsin L, IL-17 and guanylate binding protein (GBP)-2] that are up regulated by SEB. Quiflapon sodium (MK591) undergoes apoptosis within hours of treatment. Quiflapon sodium also induces rapid activation of the stress kinase, c-Jun N-terminal kinase (JNK), which plays an important role in the apoptosis process. Quiflapon sodium triggers apoptosis in prostate cancer cells without inhibition of PI3K-Akt, or ERK. Moreover, Quiflapon sodium and LY294002 exert synergistic effect in inducing apoptosis in prostate cancer cells. Quiflapon sodium (MK591) influences cAMP response element-binding protein but not Sp1.

Hyperoxia groups of mice treated with Quiflapon sodium (MK591) (20, 40 mg/kg) show alveolarization that resembles that of room air controls while untreated hyperoxia groups show definite evidence of aberrant alveolarization but no inflammation. Comparison of the Aβ-immunopositive areas between the placebo and Quiflapon sodium (MK591) (320 mg/kg)-treated group reveals a statistically significant reduction of the amyloid burden in the treated mice. Quiflapon sodium also has a significant reduction in brain levels of IL-1β. Mice treated with Quiflapon sodium show a statistically significant decrease in the steady-state levels of total CREB and its phosphorylated form at Ser133.

Quiflapon sodium | MK-0591 | L-686708

Immunology/Inflammation

FLAP

FLAP

Inflammation/Immunology

Asthma

147030-01-1

609.1531

C34H34ClN2NaO3S

>98% (HPLC)

10 mM in DMSO

CC(C)(C)SC1=C(N(C2=C1C=C(C=C2)OCC3=NC4=CC=CC=C4C=C3)CC5=CC=C(C=C5)Cl)CC(C)(C)C(=O)[O-].[Na+]

1H-Indole-2-propanoic acid, 1-[(4-chlorophenyl)methyl]-3-[(1,1-dimethylethyl)thio]-α,α-dimethyl-5-(2-quinolinylmethoxy)-, sodium salt (1:1)

(-20℃)

With Ice Pack

≥ 2 years