1144035-53-9 Usage
Uses
Different sources of media describe the Uses of 1144035-53-9 differently. You can refer to the following data:
1. PF8380 is a novel autotaxin inhibitor which reduces lysophosphatidic acid levels in plasma and at the site of inflammation.
2. 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.
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.
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.
