中文名称:

马来酸哌克昔林

中文同义词:

马来酸哌西林;肉碱棕榈酰转移酶1抑制剂(PERHEXILINE MALEATE);马来酸哌克昔林

英文名称:

PERHEXILINE MALEATE SALT

英文同义词:

2-(2,2-dicyclohexylethyl)piperidinemaleate;2-(2,2-dicyclohexylethyl)-piperidinmaleate(1:1);perhexilinemaleate;perhexilene maleate;Pexid;WSM-3978;rac Perhexiline Maleate;2-(2,2-dicyclohexylethyl)piperidinium hydrogen maleate

CAS号:

6724-53-4

分子式:

C23H39NO4

分子量:

393.56

EINECS号:

229-775-5

相关类别:

细胞生物学试剂;Heterocycles;Intermediates Fine Chemicals;Pharmaceuticals;THENYLENE

Mol文件:

6724-53-4.mol

熔点 

181-183°C

储存条件 

2-8°C

溶解度 

DMSO: ≥5mg/mL

形态

powder

颜色

white to tan

生物活性

Perhexiline maleate 是一种有效的 carnitine palmitoyltransferase 1 (CPT1) 的抑制剂，对大鼠心脏CPT1和肝脏CPT1的IC50值分别为77 μM和148 μM。

靶点

Target Value rat heart CPT1 (Cell-free assay) 77 μM rat liver CPT1 (Cell-free assay) 148 μM

Target

Value

rat heart CPT1 (Cell-free assay)

77 μM

rat liver CPT1 (Cell-free assay)

148 μM

体外研究

At 24, 48 and 72 h of treatment with 0.01 and 1 μM of Perhexiline , NDM29 ncRNA expression level in SH-SY5Y cells is progressively increased, reaching a peak after 48 hours of treatment. Perhexiline treatment increases the susceptibility of NB cells to antiblastic treatments. Co-administration of Perhexiline maleate potentiates the efficacy of cisplatin to reduce the in vitro clonogenic potential of NB cells.

体内研究

The co-administration of Perhexiline and cisplatin yields a clear enhancement of antitumor effects, resulting in a significantly improved progression-free survival as compared with mice treated with DMSO. Perhexiline favors NB cell transition to differentiated phenotype.

WGK Germany 

2

RTECS号

TM7068000

毒性

LD50 in rats, mice (g/kg): >7, 4.37 orally (Causa, Perri)