CAS 1144035-53-9; pf-8380

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CAS:

1144035-53-9

分子式:

C₂₂H₂₁Cl₂N₃O₅

分子量:

478.33

英文名称:

pf-8380

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

4-[3-(2,3-dihydro-2-oxo-6-benzoxazolyl)-3-oxopropyl]-1-piperazinecarboxylic acid (3,5-dichlorophenyl)methyl ester

用途:

PF-8380是高活性的autotaxin特异性抑制剂，IC50为2.8nM。

推荐供应商

货号

品牌

产品名称

规格

包装、参考价格

详情

P864340

MACKLIN

PF-8380

≥98%

436元/5mg;

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储存：-20°C

P797199

MACKLIN

PF-8380

10mM in DMSO

648元/1ml;

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储存：-20°C

SML0715

Sigma-Aldrich

PF-8380

≥98% (HPLC)

1117.23元/5 MG; 4498.97元/25 MG;

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产品说明

应用

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.

包装

5, 25 mg in glass bottle

生化/生理作用

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.
PF-8380 is a potent orally bioavailable inhibitor of autotaxin (ATX), the enzyme that synthesize lysophosphatidic acid (LPA) from lysophosphatidyl choline, and is an emerging target for treatment of inflammatory conditions, including cancer, arthritis and multiple sclerosis. PF-8380 blocks inflammation-induced LPA synthesis. PF-8380 works both in vitro and in vivo through direct inhibition of autotaxin. In human whole blood PF-8380 inhibited autotaxin with an IC₅₀ of 101 nM.

基本信息

经验(实验)分子式	C₂₂H₂₁Cl₂N₃O₅
分子量	478.33
NACRES	NA.77

产品性质

质量水平	100
测定	≥98% (HPLC)
形式	powder
颜色	white to beige
溶解性	DMSO: 5 mg/mL, clear (warmed)
储存温度	−20℃

安全信息

储存分类代码	13 - Non Combustible Solids
WGK	WGK 3
闪点(F)	Not applicable
闪点(C)	Not applicable

189512

Sigma-Aldrich

Autotaxin Inhibitor III, PF-8380-CAS 1144035-53-9-Calbiochem

The Autotaxin Inhibitor III, PF-8380, also referenced under CAS 1144035-53-9, controls the biological activity of Autotaxin. This small molecule/inhibitor is primarily used for Membrane applications.

3352.28元/10 MG;

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产品说明

一般描述

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.).

包装

10 mg in Glass bottle
Packaged under inert gas

警告

Toxicity: Standard Handling (A)

重悬

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

其他说明

Gierse, J., et al. 2010. J. Pharmacol. Exp. Ther.334, 310.

法律信息

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

基本信息

经验(实验)分子式	C₂₂H₂₁Cl₂N₃O₅
分子量	478.33
MDL编号	MFCD20527274

产品性质

质量水平	100
测定	≥95% (HPLC)
形式	powder
manufacturer/tradename	Calbiochem^®
储存条件	OK to freeze protect from light
颜色	tan
溶解性	DMSO: 100 mg/mL
运输	dry ice
储存温度	−20℃
SMILES string	O=C(OCC1=CC(Cl)=CC(Cl)=C1)N2CCN(CCC(C3=CC(OC(N4)=O)=C4C=C3)=O)CC2

安全信息

储存分类代码	11 - Combustible Solids
WGK	WGK 3
闪点(F)	Not applicable
闪点(C)	Not applicable

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