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HomeProduct name list4-[3-Oxo-3-(2-oxo-2,3-dihydrobenzoxazol-6-yl)propyl]piperazine-1-carboxylic acid 3,5-dichlorobenzyl ester

4-[3-Oxo-3-(2-oxo-2,3-dihydrobenzoxazol-6-yl)propyl]piperazine-1-carboxylic acid 3,5-dichlorobenzyl ester

Synonym(s):4-[3-(2,3-Dihydro-2-oxo-6-benzoxazolyl)-3-oxopropyl]-1-piperazinecarboxylic acid (3,5-dichlorophenyl)methyl ester;4-[3-Oxo-3-(2-oxo-2,3-dihydrobenzoxazol-6-yl)propyl]piperazine-1-carboxylic acid 3,5-dichlorobenzyl ester;6-(3-(Piperazin-1-yl)propanoyl)-benzo[d]oxazol-2(3H)-one, Atx Inhibitor III, PF-8380;Autotaxin Inhibitor III, PF-8380 - CAS 1144035-53-9 - Calbiochem

4-[3-Oxo-3-(2-oxo-2,3-dihydrobenzoxazol-6-yl)propyl]piperazine-1-carboxylic acid 3,5-dichlorobenzyl ester Structural

What is 4-[3-Oxo-3-(2-oxo-2,3-dihydrobenzoxazol-6-yl)propyl]piperazine-1-carboxylic acid 3,5-dichlorobenzyl ester?

The Uses of 4-[3-Oxo-3-(2-oxo-2,3-dihydrobenzoxazol-6-yl)propyl]piperazine-1-carboxylic acid 3,5-dichlorobenzyl ester

PF8380 is a novel autotaxin inhibitor which reduces lysophosphatidic acid levels in plasma and at the site of inflammation.

The Uses of 4-[3-Oxo-3-(2-oxo-2,3-dihydrobenzoxazol-6-yl)propyl]piperazine-1-carboxylic acid 3,5-dichlorobenzyl ester

PF-8380 has been used in biological assays. It has also been used to estimate the role of intestinally-derived lysophosphatidic acid in dyslipidemia and atherosclerosis.

What are the applications of Application

PF-8380 is a substrate competitive and tight-binding inhibitor of autotaxin

General Description

An orally bioavailable piperazinylbenzoxazolone compound that acts as a substrate competitive and tight-binding inhibitor of autotaxin activity {IC50 = 2.8 and 1.7 nM for recombinant human enzyme-β isoform employing FS-3 and LPC (lysophosphatidylcholine) as substrates, respectively; 1.16 and 1.15 nM for rat/murine enzyme-FS-3 and fetal fibroblast cell-LPC; 101 nM for human whole blood}. Displays desirable pharmacokinetics properties and efficiently blocks inflammation-induced LPA (lysophosphatidic acid) production both in plasma and at the site of inflammation by 95% in rat adjuvant-induced arthritis model (30 mg/kg, p.o.).

Biological Activity

pf-8380 is a specific and potent inhibitor of autotaxin (atx) with an ic50 value of 2.8 nm [1].autotaxin (atx) is a secreted enzyme having lysophospholipase d activity

Biochem/physiol Actions

PF-8380 [6-(3-(piperazin-1-yl)propanoyl)benzo[d]oxazol-2(3H)-one] has the ability to change the resistant and invasive features of glioblastoma and helps to improve the response to radiation therapy.

Properties of 4-[3-Oxo-3-(2-oxo-2,3-dihydrobenzoxazol-6-yl)propyl]piperazine-1-carboxylic acid 3,5-dichlorobenzyl ester

Density  1.419
storage temp.  -20°C
solubility  DMSO: soluble5mg/mL, clear (warmed)
form  Tan powder
pka 8.74±0.70(Predicted)
color  white to beige

Safety information for 4-[3-Oxo-3-(2-oxo-2,3-dihydrobenzoxazol-6-yl)propyl]piperazine-1-carboxylic acid 3,5-dichlorobenzyl ester

Signal word Warning
Pictogram(s)
ghs
Exclamation Mark
Irritant
GHS07
GHS Hazard Statements H302:Acute toxicity,oral
H315:Skin corrosion/irritation
H319:Serious eye damage/eye irritation
H335:Specific target organ toxicity, single exposure;Respiratory tract irritation
H413:Hazardous to the aquatic environment, long-term hazard
Precautionary Statement Codes P261:Avoid breathing dust/fume/gas/mist/vapours/spray.
P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

Computed Descriptors for 4-[3-Oxo-3-(2-oxo-2,3-dihydrobenzoxazol-6-yl)propyl]piperazine-1-carboxylic acid 3,5-dichlorobenzyl ester

InChIKey JMSUDQYHPSNBSN-UHFFFAOYSA-N

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