4-[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 Structure](CAS/GIF/1144035-53-9.gif)
- 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; 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;3,5-Dichlorobenzyl 4-(3-oxo-3-(2-oxo-2,3-dihydrobenzo[d]oxazol-6-yl)propyl)piperazine-1-ca.
- CBNumber:
- CB52589638
- Molecular Formula:
- C22H21Cl2N3O5
- Molecular Weight:
- 478.33
- MDL Number:
- MFCD20527274
- MOL File:
- 1144035-53-9.mol
- MSDS File:
- SDS
4-[3-Oxo-3-(2-oxo-2,3-dihydrobenzoxazol-6-yl)propyl]piperazine-1-carboxylic acid 3,5-dichlorobenzyl ester Properties
| 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 |
| InChIKey | JMSUDQYHPSNBSN-UHFFFAOYSA-N |
| FDA UNII | T582DIM5A4 |
| UNSPSC Code | 51111800 |
| NACRES | NA.77 |
SAFETY
Risk and Safety Statements
| Symbol(GHS) |  GHS07 |
|---|---|
| Signal word | Warning |
| Hazard statements | H302-H315-H319-H335-H413 |
| Precautionary statements | P261-P305+P351+P338 |
| WGK Germany | 3 |
4-[3-Oxo-3-(2-oxo-2,3-dihydrobenzoxazol-6-yl)propyl]piperazine-1-carboxylic acid 3,5-dichlorobenzyl ester price More Price(30)
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Sigma-Aldrich | SML0715 | PF-8380 ≥98% (HPLC) | 1144035-53-9 | 5mg | $125 | 2024-03-01 | Buy |
| Sigma-Aldrich | 189512 | Autotaxin Inhibitor III, PF-8380 | 1144035-53-9 | 10mg | $259 | 2024-03-01 | Buy |
| Cayman Chemical | 12018 | PF-8380 ≥95% | 1144035-53-9 | 1mg | $48 | 2024-03-01 | Buy |
| Cayman Chemical | 12018 | PF-8380 ≥95% | 1144035-53-9 | 5mg | $131 | 2024-03-01 | Buy |
| Sigma-Aldrich | SML0715 | PF-8380 ≥98% (HPLC) | 1144035-53-9 | 25mg | $478 | 2024-03-01 | Buy |
4-[3-Oxo-3-(2-oxo-2,3-dihydrobenzoxazol-6-yl)propyl]piperazine-1-carboxylic acid 3,5-dichlorobenzyl ester Chemical Properties,Uses,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
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 33024 | 60 |
| BOC Sciences | +1-631-485-4226 | inquiry@bocsci.com | United States | 19552 | 58 |
| Alchem Pharmtech,Inc. | 8485655694 | sales@alchempharmtech.com | United States | 63687 | 58 |
| CONIER CHEM AND PHARMA LIMITED | +8618523575427 | sales@conier.com | China | 49732 | 58 |
| career henan chemical co | +86-0371-86658258 +8613203830695 | factory@coreychem.com | China | 29808 | 58 |
| TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | marketing@targetmol.com | United States | 32159 | 58 |
| HANGZHOU CLAP TECHNOLOGY CO.,LTD | 86-571-88216897,88216896 13588875226 | sales@hzclap.com | CHINA | 6312 | 58 |
| Hefei Hirisun Pharmatech Co., Ltd | +8615056975894 | shawn@hirisunpharm.com | CHINA | 9911 | 58 |
| Zhejiang J&C Biological Technology Co.,Limited | +1-2135480471 +1-2135480471 | sales@sarms4muscle.com | China | 10473 | 58 |
| InvivoChem | +1-708-310-1919 +1-13798911105 | sales@invivochem.cn | United States | 6391 | 58 |
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
| Image | Update time | Product | Price | Min. Order | Purity | Supply Ability | Manufacturer | |
|---|---|---|---|---|---|---|---|---|
 |
2024-11-19 | PF-8380
1144035-53-9
|
US $38.00-137.00 / mg | 99.45% | 10g | TargetMol Chemicals Inc. | ||
![4-[3-Oxo-3-(2-oxo-2,3-dihydrobenzoxazol-6-yl)propyl]piperazine-1-carboxylic acid 3,5-dichlorobenzyl ester pictures](https://img.chemicalbook.com/ProductImageEN/2020-1/Small/9dd44a88-4324-4f38-8353-d4de078758bb.png) |
2020-01-14 | 4-[3-Oxo-3-(2-oxo-2,3-dihydrobenzoxazol-6-yl)propyl]piperazine-1-carboxylic acid 3,5-dichlorobenzyl ester
1144035-53-9
|
US $9.80 / KG | 1g | ≥99% | 100kg | Career Henan Chemical Co |
-
- PF-8380
1144035-53-9
- US $38.00-137.00 / mg
- 99.45%
- TargetMol Chemicals Inc.
-
- 4-[3-Oxo-3-(2-oxo-2,3-dihydrobenzoxazol-6-yl)propyl]piperazine-1-carboxylic acid 3,5-dichlorobenzyl ester
1144035-53-9
- US $9.80 / KG
- ≥99%
- Career Henan Chemical Co
4-[3-Oxo-3-(2-oxo-2,3-dihydrobenzoxazol-6-yl)propyl]piperazine-1-carboxylic acid 3,5-dichlorobenzyl ester Spectrum
1144035-53-9(4-[3-Oxo-3-(2-oxo-2,3-dihydrobenzoxazol-6-yl)propyl]piperazine-1-carboxylic acid 3,5-dichlorobenzyl ester)Related Search:
1of4