Synonyms: 1-Cyclopropyl-4-[4-[[5-methyl-3-[3-[4-(trifluoromethoxy)phenyl]-1,2,4-oxadiazol-5-yl]-1H-pyrazol-1-yl]methyl]-2-pyridinyl]piperazine; 1-Cyclopropyl-4-{4-[(5-methyl-3-{3-[4-(trifluoromethoxy)phenyl]-1,2,4-oxadiazol-5-yl}-1H-pyrazol-1-yl)methyl]pyridin-2-yl}piperazine
Molecular Formula: C26H26F3N7O2
Molecular Weight: 525.53
Linear Structural Formula: C26H26F3N7O2
MDL Number: MFCD28143915
Purity: >=98% (HPLC)
Storage: 2-8C
Biochem Physiol Actions: BAY 87-2243 is an orally active oxidative phosphorylation (OxPhos) inhibitor that potently suppresses hypoxia-induced HIF-1 activation (IC50 = 0.7 nM by HCT-116-based reporter assay; 24 h 1% O2) by selectively targeting mitochondrial complex I (IC50 = 10 nM using mitochondria from PC3; no inhibition of complex III), exhibiting antiproliferation activity in cancer cultures only in the absence of glucose (IC50 >=3 nM in H460 cultures with 10 mM galactose or lactate, >10 muM with 10 mM glucose). BAY 87-2243 selectively inhibits hypoxia-induced, but not hypoxia-independent, HIF-1alpha & HIF-2alpha upregulation and HIF-1 target genes expression in cultures (IC50 <=10 nM/ADM, ANGPTL4, CA9 mRNA in H460 cells; IC50 = 2 nM/carbonic anhydrase 9 (CA9) protein in HCT116 cells) and effectively suppresses H460 xenograft tumor growth in mice via daily oral admiminstration in vivo (ED50 >=2 mg/kg).