N/A

中文名称:

N/A

中文同义词:

ATX(AUTOTAXIN)抑制剂(HA130)

英文名称:

HA 130

英文同义词:

B-[3-[[4-[[3-[(4-Fluorophenyl)Methyl]-2,4-dioxo-5-thiazolidinylidene]Methyl]phenoxy]Methyl]phenyl]boronic Acid;HA130 (Autotaxin Inhibitor);HA 130;HA 150;HA130 (HA-130);(Z)-3-((4-((3-(4-fluorobenzyl)-2,4-dioxothiazolidin-5-ylidene)methyl)phenoxy)methyl)phenylboronic acid;CS-1606;HA130;HA-130;HA 130

CAS号:

1229652-21-4

分子式:

C24H19BFNO5S

分子量:

463.29

EINECS号:

相关类别:

细胞生物学试剂;小分子抑制剂;小分子抑制剂，天然产物;Aromatics, Boron Derivatives, Heterocycles, Inhibitors, Pharmaceuticals, Intermediates Fine Chemicals;Aromatics;Boron Derivatives;Heterocycles;Inhibitors;Intermediates Fine Chemicals;Pharmaceuticals;Selective autotaxin inhibitor.

Mol文件:

1229652-21-4.mol

生物活性

HA130 是一种选择性的 autotaxin (ATX) 抑制剂，IC50 为 28 nM。

靶点

Autotaxin 28 nM (IC 50 )

Autotaxin 28 nM (IC 50 )

体外研究

HA130 completely blocks the ability of ATX to promote TEM (transendothelial migration). HA130 at 0.3 μM completely ablates the activity of ATX on TK1 uropod formation.

体内研究

HA130 slows T cell migration across lymph node HEVs. HA130 decreases the "outside HEVs/inside HEVs" ratio by 3-4-fold compared to vehicle-treated animals vehicle. The s.c. administration of HA130 induces marked lymphocyte accumulation within the endothelial cell (EC) and sub-EC layers of HEVs in draining lymph nodes (LNs).