BRP-7

BRP-7 is a 5-lipoxygenase activating protein (FLAP) inhibitor with an IC50 of 0.31 μM. BRP-7 inhibits the co-localization of 5-lipoxygenase (5-LOX) and FLAP by targeting FLAP, thereby blocking the transfer of arachidonic acid (AA) to 5-LOX and suppressing the production of leukotrienes (LTs) (IC₅₀ = 0.15 μM) . BRP-7 does not inhibit cyclooxygenase (COX-1/COX-2) or microsomal prostaglandin E₂ synthase-1 (mPGES-1), and does not affect cell viability or AA release. BRP-7 exhibits significant anti-inflammatory effects in rat pleurisy and mouse peritonitis models. BRP-7 can be used for the study of inflammatory diseases[1][2].

Product Specifications

CAS Number

[612046-20-5]

UNSPSC

12352005

Target

FLAP

Related Pathways

Immunology/Inflammation

Applications

COVID-19-immunoregulation

Field of Research

Inflammation/Immunology

Smiles

ClC1=C(CN2C3=C(N=C2C(C)C4=CC=C(CC(C)C)C=C4)C=CC=C3)C=CC=C1

Molecular Formula

C26H27ClN2

Molecular Weight

402.96

References & Citations

[1]Gür ZT, et al. Identification of multi-target inhibitors of leukotriene and prostaglandin E2 biosynthesis by structural tuning of the FLAP inhibitor BRP-7. Eur J Med Chem. 2018 Apr 25;150:876-899.|[2]Pergola C, et al. The novel benzimidazole derivative BRP-7 inhibits leukotriene biosynthesis in vitro and in vivo by targeting 5-lipoxygenase-activating protein (FLAP) . Br J Pharmacol. 2014 Jun;171 (12) :3051-64.