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BI 665915

Names

[ CAS No. ]:
1360550-04-4

[ Name ]:
BI 665915

[Synonym ]:
MFCD28902241
1H-Pyrazole-1-acetamide, 4-[3-[(1R)-1-[4-(2-amino-5-pyrimidinyl)phenyl]-1-cyclopropylethyl]-1,2,4-oxadiazol-5-yl]-N,N-dimethyl-
2-[4-(3-{(1R)-1-[4-(2-Amino-5-pyrimidinyl)phenyl]-1-cyclopropylethyl}-1,2,4-oxadiazol-5-yl)-1H-pyrazol-1-yl]-N,N-dimethylacetamide

Biological Activity

[Description]:

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 LTB4production in vivo.

[References]

References 1. Takahashi H, et al. J Med Chem. 2015 Feb 26;58(4):1669-90. View Related Products by Target FLAP

Chemical & Physical Properties

[ Density]:
1.4±0.1 g/cm3

[ Boiling Point ]:
738.8±70.0 °C at 760 mmHg

[ Molecular Formula ]:
C24H26N8O2

[ Molecular Weight ]:
458.516

[ Flash Point ]:
400.6±35.7 °C

[ Exact Mass ]:
458.217865

[ LogP ]:
1.75

[ Vapour Pressure ]:
0.0±2.4 mmHg at 25°C

[ Index of Refraction ]:
1.717

Related Compounds