SML2870

BI 99179

≥98% (HPLC)

• Synonym(e): (1R,3S)-3-Propionylaminocyclopentanecarboxylic acid N-[4-(benzoxazol-2-yl)phenyl]-N-methylamide, (1R,3S)-N-[4-(2-Benzoxazolyl)phenyl]-N-methyl-3-[(1-oxopropyl)amino]cyclopentanecarboxamide, BI99179
• Empirische Formel (Hill-System): C₂₃H₂₅N₃O₃
• CAS-Nummer: 1291779-76-4
• Molekulargewicht: 391.46
• MDL-Nummer: MFCD25976795
• UNSPSC-Code: 12352200

Eigenschaften

• Qualitätsniveau: 100
• Assay: ≥98% (HPLC)
• Form: powder
• Farbe: white to beige
• Löslichkeit: DMSO: 2 mg/mL, clear
• Lagertemp.: −20°C
• SMILES String: CCC(N[C@H]1CC[C@@H](C(N(C)C2=CC=C(C=C2)C3=NC4=C(O3)C=CC=C4)=O)C1)=O

Beschreibung

Biochem./physiol. Wirkung

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% inhibition at 10 μM) and human CYP450 isoenzymes (1A2/2C9/2C19/2D6/3A4 IC₅₀ >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).

Sicherheitshinweise

• Lagerklassenschlüssel: 11 - Combustible Solids
• WGK: WGK 3