| Identification | Back Directory | [Name]
VU 0364739 HYDROCHLORIDE | [CAS]
1244640-48-9 | [Synonyms]
VU0364739 HCl
N-[2-[1-(3-Fluorophenyl)-4-oxo-1,3,8-triazaspiro[4.5]dec-8-yl]ethyl]-2-naphthalenecarboxamide | [Molecular Formula]
C26H28ClFN4O2 | [MDL Number]
MFCD19690943 | [MOL File]
1244640-48-9.mol | [Molecular Weight]
482.98 |
| Hazard Information | Back Directory | [Uses]
VU 0364739 Hydrochloride is a selective, small molecule inhibitor of phopholipase D2. | [Biological Activity]
PLD2-selectivePH domain-targeting phospholipase D allosteric inhibitor with in vitro and in vivo efficacy.
VU0364739 is a PLD2-selectivePH 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 μMrespectively). VU0364739 is reported to suppress PLD2-dependent proliferation in cultures (by 56% in 48 hrs; MDA-MB-23110 μM) and alleviate the symptoms of DSS-induced colitis in mice in vivo (10 mg/kg i.p. qod). | [in vivo]
1.19 Pharmacokinetic 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 50]
PLD2: 20 nM (IC50); PLD1: 1500 nM (IC50) | [storage]
Desiccate at RT |
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| Company Name: |
BOC Sciences
|
| Tel: |
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| Website: |
https://www.bocsci.com |
| Company Name: |
cjbscvictory
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| Tel: |
13348960310 |
| Website: |
https://www.weikeqi-biotech.com/ |
| Company Name: |
Merck KGaA
|
| Tel: |
21-20338288 |
| Website: |
www.sigmaaldrich.cn |
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