1144035-53-9 Usage
Description
4-[3-Oxo-3-(2-oxo-2,3-dihydrobenzoxazol-6-yl)propyl]piperazine-1-carboxylic acid 3,5-dichlorobenzyl ester is an orally bioavailable piperazinylbenzoxazolone compound that acts as a substrate competitive and tight-binding inhibitor of autotaxin activity. It has a low IC50 value for recombinant human enzyme-β isoform and rat/murine enzyme-FS-3, as well as fetal fibroblast cell-LPC, indicating its high potency and selectivity. 4-[3-Oxo-3-(2-oxo-2,3-dihydrobenzoxazol-6-yl)propyl]piperazine-1-carboxylic acid 3,5-dichlorobenzyl ester also displays desirable pharmacokinetic properties and efficiently blocks inflammation-induced lysophosphatidic acid (LPA) production both in plasma and at the site of inflammation.
Uses
Used in Autotaxin Inhibition:
4-[3-Oxo-3-(2-oxo-2,3-dihydrobenzoxazol-6-yl)propyl]piperazine-1-carboxylic acid 3,5-dichlorobenzyl ester is used as an autotaxin inhibitor for reducing lysophosphatidic acid levels in plasma and at the site of inflammation. This makes it a potential therapeutic agent for treating inflammatory diseases and conditions.
Used in Biological Assays:
4-[3-Oxo-3-(2-oxo-2,3-dihydrobenzoxazol-6-yl)propyl]piperazine-1-carboxylic acid 3,5-dichlorobenzyl ester is also used in biological assays to study the role of autotaxin and lysophosphatidic acid in various biological processes and diseases.
Used in Dyslipidemia and Atherosclerosis Research:
4-[3-Oxo-3-(2-oxo-2,3-dihydrobenzoxazol-6-yl)propyl]piperazine-1-carboxylic acid 3,5-dichlorobenzyl ester has been used to estimate the role of intestinally-derived lysophosphatidic acid in dyslipidemia and atherosclerosis, providing insights into the potential therapeutic applications of targeting autotaxin in these conditions.
Used in Inflammation-Induced LPA Production Blockage:
In the rat adjuvant-induced arthritis model, this compound efficiently blocks inflammation-induced LPA production both in plasma and at the site of inflammation by 95% at a dosage of 30 mg/kg, making it a promising candidate for the treatment of inflammatory disorders.
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.
Check Digit Verification of cas no
The CAS Registry Mumber 1144035-53-9 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,1,4,4,0,3 and 5 respectively; the second part has 2 digits, 5 and 3 respectively.
Calculate Digit Verification of CAS Registry Number 1144035-53:
(9*1)+(8*1)+(7*4)+(6*4)+(5*0)+(4*3)+(3*5)+(2*5)+(1*3)=109
109 % 10 = 9
So 1144035-53-9 is a valid CAS Registry Number.
1144035-53-9Relevant articles and documents
A novel autotaxin inhibitor reduces lysophosphatidic acid levels in plasma and the site of inflammation
, p. 310 - 317 (2010)
Autotaxin is the enzyme responsible for the production of lysophosphatidic acid (LPA) from lysophosphatidyl choline (LPC), and it is up-regulated in many inflammatory conditions, including but not limited to cancer, arthritis, and multiple sclerosis. LPA
PIPERIDINE AND PIPERAZINE DERIVATIVES
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Page/Page column 29, (2010/09/07)
Compounds of the formula (I), in which R1, R2, R3, D, G, Q and W have the meanings indicated in claim (1), can and be employed for the treatment of tumours.
