1291779-76-4

1291779-76-4 structure

Name: BI99179
Chemical Name: (1R,3S)-N-[4-(1,3-Benzoxazol-2-yl)phenyl]-N-methyl-3-(propionylamino)cyclopentanecarboxamide
CAS Number: 1291779-76-4
Molecular Formula: C₂₃H₂₅N₃O₃
Molecular Weight: 391.463
Catalog: Signaling Pathways Metabolic Enzyme/Protease Fatty Acid Synthase (FAS)
Create Date: 2020-01-12 00:35:59
Modify Date: 2024-04-05 15:59:07
BI-99179 is a potent and selective inhibitor of type I fatty acid synthase (FAS) with IC50 of 79 nM; demonstrates potent cellular activity (inhibition of 14C-acetate incorporation) with IC50 of 0.6 uM in the mouse N-42 cellular assays, shows no significant LDH release in the cytotoxicity assay at >30 uM; BI-99179 is a tool compound suitable for the in vivo validation of FAS as a therapeutic target.

Name	(1R,3S)-N-[4-(1,3-Benzoxazol-2-yl)phenyl]-N-methyl-3-(propionylamino)cyclopentanecarboxamide
Synonyms	Cyclopentanecarboxamide, N-[4-(2-benzoxazolyl)phenyl]-N-methyl-3-[(1-oxopropyl)amino]-, (1R,3S)- (1R,3S)-N-[4-(1,3-Benzoxazol-2-yl)phenyl]-N-methyl-3-(propionylamino)cyclopentanecarboxamide

Description	BI-99179 is a potent and selective inhibitor of type I fatty acid synthase (FAS) with IC50 of 79 nM; demonstrates potent cellular activity (inhibition of 14C-acetate incorporation) with IC50 of 0.6 uM in the mouse N-42 cellular assays, shows no significant LDH release in the cytotoxicity assay at >30 uM; BI-99179 is a tool compound suitable for the in vivo validation of FAS as a therapeutic target.
Related Catalog	Research Areas >> Cancer Signaling Pathways >> Metabolic Enzyme/Protease >> Fatty Acid Synthase (FAS) Research Areas >> Metabolic Disease
Target	IC50: 79 nM (FAS)[1]
In Vitro	BI 99179 is potent in the mouse hypothalamic N-42 cell with an IC50 of 0.6 μM. BI 99179 shows no significant LDH release in the cytotoxicity assay up to 30 μM[1].
In Vivo	BI 99179 has a super pharmacokinetic profile in male Han/Wistar rats (oral application of 4 mg/kg)with half life (t1/2) of 3.0 h[1].
References	[1]. Kley JT, et al. Discovery of BI 99179, a potent and selective inhibitor of type I fatty acid synthase with central exposure.Bioorg Med Chem Lett. 2011 Oct 1;21(19):5924-7.