612046-20-5
Chemical Structure
BRP-7
- CAS No.: 612046-20-5
- Formula:C26H27ClN2
- Molecular Weight:402.96
IUPAC Name: 1-(2-chlorobenzyl)-2-(1-(4-isobutylphenyl)ethyl)-1H-benzo[d]imidazole
InChIKey: RSOFSWHYZCGXSL-UHFFFAOYSA-N
SMILES: ClC1=C(CN2C3=C(N=C2C(C)C4=CC=C(CC(C)C)C=C4)C=CC=C3)C=CC=C1
Biological Activity:
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].
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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. |
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References
- [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. [Content Brief]
- [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.
