Synonyms: N-(2-(4-Oxo-1-phenyl-1,3,8-triazaspiro[4.5]decan-8-yl)ethyl)-2-naphthamide; N-(2-(4-Oxo-1-phenyl-1,3,8-triazaspiro[4.5]decan-8-yl)ethyl)naphthalene-2-carboxamide; N-[2-(4-Oxo-1-phenyl-1,3,8-triazaspiro[4.5]dec-8-yl)ethyl]-2-naphthalenecarboxamide; NOPT; VU0155072-2
Molecular Formula: C26H28N4O2
Molecular Weight: 428.53
Linear Structural Formula: C26H28N4O2
MDL Number: MFCD18382100
Purity: >=98% (HPLC)
Storage: 2-8C
Biochem Physiol Actions: VU0155072 is a PLD2-selective, PH domain-targeting allosteric phospholipase D inhibitor (human PLD2/PLD1 IC50 = 140 nM/5.1 μM vs. PH/PX-deleted rat PLD1 IC50 >20 μM; cellular PLD IC50 = 110 nM/GFP-PLD2-overexpressing HEK293 vs. 1 μM/PMA-stimulated Calu-1 with predominant PLD1 activity) that selectively suppresses PLD2-dependent MDA-MB-231 invasion in cultures (by 60% in 48 hrs; 200 nM) and exhibits in vivo efficacy in murine models of DSS-induced colitis (4 mg/kg/day p.o.) and breast tumor-associated macrophages/neutrophils infiltration (75 μg/0.11 μL/kg/hr via osmotic pump). Use low concentrations (<5 μm) for cell treatment to avoid dual pld1 inhibition.<>5>