4-[3-Oxo-3-(2-oxo-2,3-dihydrobenzoxazol-6-yl)propyl]piperazine-1-carboxylic acid 3,5-dichlorobenzyl ester
- Product Name
- 4-[3-Oxo-3-(2-oxo-2,3-dihydrobenzoxazol-6-yl)propyl]piperazine-1-carboxylic acid 3,5-dichlorobenzyl ester
- CAS No.
- 1144035-53-9
- Chemical Name
- 4-[3-Oxo-3-(2-oxo-2,3-dihydrobenzoxazol-6-yl)propyl]piperazine-1-carboxylic acid 3,5-dichlorobenzyl ester
- Synonyms
- CS-894;PF 8380;PF-8380 HCL;PF-8380 ，S8218;PF 8380; PF8380;PF-8380, ATX Inhibitor;PF-8380;PF 8380;PF8380;PF-8380, 10 mM in DMSO;Autotaxin Inhibitor III, PF-8380;Autotaxin Inhibitor III, PF-8380 - CAS 1144035-53-9 - Calbiochem
- CBNumber
- CB52589638
- Molecular Formula
- C22H21Cl2N3O5
- Formula Weight
- 478.33
- MOL File
- 1144035-53-9.mol
4-[3-Oxo-3-(2-oxo-2,3-dihydrobenzoxazol-6-yl)propyl]piperazine-1-carboxylic acid 3,5-dichlorobenzyl ester Property
- 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
- InChI
- InChI=1S/C22H21Cl2N3O5/c23-16-9-14(10-17(24)12-16)13-31-22(30)27-7-5-26(6-8-27)4-3-19(28)15-1-2-18-20(11-15)32-21(29)25-18/h1-2,9-12H,3-8,13H2,(H,25,29)
- InChIKey
- JMSUDQYHPSNBSN-UHFFFAOYSA-N
- SMILES
- N1(C(OCC2=CC(Cl)=CC(Cl)=C2)=O)CCN(CCC(C2C=C3OC(=O)NC3=CC=2)=O)CC1
Safety
- WGK Germany
- 3
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
H413May cause long lasting harmful effects to aquatic life
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
N-Bromosuccinimide Price
- Product number
- SML0715
- Product name
- PF-8380
- Purity
- ≥98% (HPLC)
- Packaging
- 5mg
- Price
- $129
- Updated
- 2025/07/31
- Product number
- 189512
- Product name
- Autotaxin Inhibitor III, PF-8380
- Packaging
- 10mg
- Price
- $226
- Updated
- 2025/07/31
- Product number
- 12018
- Product name
- PF-8380
- Purity
- ≥95%
- Packaging
- 1mg
- Price
- $48
- Updated
- 2024/03/01
- Product number
- 12018
- Product name
- PF-8380
- Purity
- ≥95%
- Packaging
- 5mg
- Price
- $131
- Updated
- 2024/03/01
- Product number
- SML0715
- Product name
- PF-8380
- Purity
- ≥98% (HPLC)
- Packaging
- 25mg
- Price
- $491
- Updated
- 2025/07/31
4-[3-Oxo-3-(2-oxo-2,3-dihydrobenzoxazol-6-yl)propyl]piperazine-1-carboxylic acid 3,5-dichlorobenzyl ester Chemical Properties,Usage,Production
Uses
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.
Uses
PF8380 is a novel autotaxin inhibitor which reduces lysophosphatidic acid levels in plasma and at the site of inflammation.
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.
in vivo
The pharmacokinetic profile of PF-8380 is evaluated at an intravenous dose of 1 mg/kg and oral doses of 1 to 100 mg/kg out to 24 h. PF-8380 has mean clearance of 31 mL/min/kg, volume of distribution at steady state of 3.2 L/kg, and effective t1/2 of 1.2 h. Oral bioavailability is moderate, ranging from 43 to 83%. Plasma concentrations increased with single oral escalating doses, but Cmax increased at a rate that is approximately proportional to dose from 1 to 10 mg/kg and less than proportional to dose from 10 to 100 mg/kg. PF-8380 exposures estimated by area under the curve are approximately proportional to dose and linear up to 100 mg/kg. Plasma C16:0, C18:0, and C20:0 LPA levels are measured immediately after collection. Maximal reduction of LPA levels is observed by the 3 mg/kg dose at 0.5 h with all LPA returning at or above baseline at 24 h[1]. Treatment with 10 mg/kg PF-8380 increases tumor-associated vascularity modestly by 20% (P=0.497). When compared to control, treatment of PF-8380 45 min before 4 Gy irradiation decreases vascularity by nearly 48% when compared to control (P=0.031) and by 65% when compared to mice that received radiation alone (P=0.011)[2].
IC 50
Autotaxin: 2.8 nM (IC50, In isolated enzyme assay)
4-[3-Oxo-3-(2-oxo-2,3-dihydrobenzoxazol-6-yl)propyl]piperazine-1-carboxylic acid 3,5-dichlorobenzyl ester Preparation Products And Raw materials
Raw materials
Preparation Products
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View Lastest Price from 4-[3-Oxo-3-(2-oxo-2,3-dihydrobenzoxazol-6-yl)propyl]piperazine-1-carboxylic acid 3,5-dichlorobenzyl ester manufacturers
- Product
- 4-[3-Oxo-3-(2-oxo-2,3-dihydrobenzoxazol-6-yl)propyl]piperazine-1-carboxylic acid 3,5-dichlorobenzyl ester 1144035-53-9
- Price
- US $9.80/KG
- Min. Order
- 1g
- Purity
- ≥99%
- Supply Ability
- 100kg
- Release date
- 2020-01-13