1291779-76-4 Usage
Biochem/physiol Actions
BI 99179 is a non-cytotoxic (by LDH release; 30 μM, U937) orally available, brain-penetrant, highly potent and selective fatty acid synthase (FAS, FASN) inhibitor (IC50 = 79 nM by cell-free human FAS assay) with little or no inhibitory potency toward a panel of 30 receptors & channels (<20%>10 μM). BI 99179 inhibits cellular FAS activity in vitro (IC50 = 180 nM/human H1975, 600 nM/murine hypothalamic N-42 cells) and increases hypothalamic [malonyl-CoA] in rats in vivo (2 h post 10 mg/kg or 2-24 hr post 100 mg/kg p.o.). Note: adverse effects in rats are reported at day 4 (30 mg/kg) and day 9 (3 mg/kg).
Check Digit Verification of cas no
The CAS Registry Mumber 1291779-76-4 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,2,9,1,7,7 and 9 respectively; the second part has 2 digits, 7 and 6 respectively.
Calculate Digit Verification of CAS Registry Number 1291779-76:
(9*1)+(8*2)+(7*9)+(6*1)+(5*7)+(4*7)+(3*9)+(2*7)+(1*6)=204
204 % 10 = 4
So 1291779-76-4 is a valid CAS Registry Number.
1291779-76-4Relevant articles and documents
Discovery of BI 99179, a potent and selective inhibitor of type i fatty acid synthase with central exposure
Kley, J?rg T.,MacK, Jürgen,Hamilton, Bradford,Scheuerer, Stefan,Redemann, Norbert
, p. 5924 - 5927 (2011/10/09)
Based on a high-throughput screen, cyclopentanecarboxanilides were identified as a new chemotype of non-covalent inhibitors of type I fatty acid synthase (FAS). Starting from initial hits we aimed at generating a tool compound suitable for the in vivo validation of FAS as a therapeutic target. Optimisation yielded BI 99179 which is characterised by high potency, remarkably high selectivity and significant exposure (both peripheral and central) upon oral administration in rats.
