SML2870
BI 99179
≥98% (HPLC)
동의어(들):
(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
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모든 사진(1)
About This Item
실험식(Hill 표기법):
C23H25N3O3
CAS Number:
Molecular Weight:
391.46
MDL number:
UNSPSC 코드:
51111800
NACRES:
NA.77
추천 제품
Quality Level
분석
≥98% (HPLC)
양식
powder
색상
white to beige
solubility
DMSO: 2 mg/mL, clear
저장 온도
−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
InChI key
YNFDIGJKJPNFFD-SJORKVTESA-N
생화학적/생리학적 작용
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).
Non-cytotoxic, orally available, brain-penetrant, highly potent and selective fatty acid synthase (FAS, FASN) inhibitor.
Storage Class Code
11 - Combustible Solids
WGK
WGK 3
가장 최신 버전 중 하나를 선택하세요:
Jörg T Kley et al.
Bioorganic & medicinal chemistry letters, 21(19), 5924-5927 (2011-08-30)
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
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