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15-LOX-1 inhibitor 1

Names

[ CAS No. ]:
2349374-37-2

[ Name ]:
15-LOX-1 inhibitor 1

[Synonym ]:
Ethyl 6-chloro-3-{(1E)-3-[(2-methoxybenzyl)amino]-3-oxo-1-propen-1-yl}-1H-indole-2-carboxylate
9c(i472)
1H-Indole-2-carboxylic acid, 6-chloro-3-[(1E)-3-[[(2-methoxyphenyl)methyl]amino]-3-oxo-1-propen-1-yl]-, ethyl ester

Biological Activity

[Description]:

15-LOX-1 inhibitor 1 is a potent inhibitor of 15-LOX-1 (15-lipoxygenase-1) with an IC50 value of 0.19 μM. 15-LOX-1 inhibitor 1 protects macrophages from lipopolysaccharide-induced cytotoxicity. 15-LOX-1 inhibitor 1 inhibits NO formation and lipid peroxidation[1].

[Related Catalog]:

Research Areas >> Inflammation/Immunology
Signaling Pathways >> Metabolic Enzyme/Protease >> 5-Lipoxygenase

[Target]

15-LOX-1:0.19 μM (IC50)


[In Vitro]

15-LOX-1 inhibitor 1 (Compound 9c) (0-5 μM; 24 hours) protects RAW 264.7 macrophages from LPS-induced cell death and shows stronger, dose-dependent effects with a 20% viability increase at 5 μM[1]. Cell Viability Assay[1] Cell Line: RAW 264.7 macrophages Concentration: 0, 0.2, 1, 5 μM 15-LOX-1 inhibitor 1 and lipopolysaccharides (LPS) (100 μg/mL) Incubation Time: 24 hours Result: Showed stronger, dose-dependent effects with a 20% viability increase at 5 μM.

[References]

[1]. Guo H, et al. Novel 15-Lipoxygenase-1 Inhibitor Protects Macrophages from Lipopolysaccharide-Induced Cytotoxicity. J Med Chem. 2019;62(9):4624-4637.

Chemical & Physical Properties

[ Density]:
1.3±0.1 g/cm3

[ Boiling Point ]:
683.5±55.0 °C at 760 mmHg

[ Molecular Formula ]:
C22H21ClN2O4

[ Molecular Weight ]:
412.866

[ Flash Point ]:
367.2±31.5 °C

[ Exact Mass ]:
412.118988

[ LogP ]:
4.74

[ Vapour Pressure ]:
0.0±2.1 mmHg at 25°C

[ Index of Refraction ]:
1.648

Related Compounds