Vu 0364739 hydrochloride

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Vu 0364739 hydrochloride Basic information
Product Name:Vu 0364739 hydrochloride
Synonyms:N-[2-[1-(3-Fluorophenyl)-4-oxo-1,3,8-triazaspiro[4.5]dec-8-yl]ethyl]-2-naphthalenecarboxamide;VU0364739 HCl;N-{2-[1-(3-fluorophenyl)-4-oxo-1,3,8-triazaspiro[4.5]decan-8-yl]ethyl}naphthalene-2-carboxamide hydrochloride
CAS:1244640-48-9
MF:C26H28ClFN4O2
MW:482.98
EINECS:
Product Categories:
Mol File:1244640-48-9.mol
Vu 0364739 hydrochloride Structure
Vu 0364739 hydrochloride Chemical Properties
storage temp. Desiccate at RT
solubility Soluble to 100 mM in DMSO
form Powder
color white to beige
Safety Information
WGK Germany WGK 3
Storage Class11 - Combustible Solids
MSDS Information
Vu 0364739 hydrochloride Usage And Synthesis
UsesVU 0364739 Hydrochloride is a selective, small molecule inhibitor of phopholipase D2.
Biological ActivityPLD2-selective, PH domain-targeting phospholipase D allosteric inhibitor with in vitro and in vivo efficacy.
VU0364739 is a PLD2-selective, PH domain-targeting phospholipase D allosteric inhibitor (PLD2/PLD1 IC50 = 100 nM/7.5 μM by enzymatic assay) th at selectively suppresses the cellular PLD activity in GFP-PLD2-overexpressing HEK293 cells over PMA-stimulated non-small-cell lung cancer (NSCLC) Calu-1 cells with predominant PLD1 activity (IC50 = 20 nM and 1.5 μM, respectively). VU0364739 is reported to suppress PLD2-dependent proliferation in cultures (by 56% in 48 hrs; MDA-MB-231, 10 μM) and alleviate the symptoms of DSS-induced colitis in mice in vivo (10 mg/kg i.p. qod).
in vivo
1.19Pharmacokinetic Properties of VU 0364739 in Rats[1].
Rats
IV 1 mg/kg		Rats
PO 10 mg/kg
CL (mL/min/kg)61.5
t1/2 (h)1.52
Vdss (L/kg)8.1
plasma (ng/mL)39.9
brain (ng/mL)29
IC 50PLD2: 20 nM (IC50); PLD1: 1500 nM (IC50)
storageDesiccate at RT
Vu 0364739 hydrochloride Preparation Products And Raw materials
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