6724-53-4
中文名稱
馬來(lái)酸哌克昔林
英文名稱
PERHEXILINE MALEATE SALT
CAS
6724-53-4
分子式
C23H39NO4
分子量
393.56
MOL 文件
6724-53-4.mol
更新日期
2024/11/05 19:25:42
6724-53-4 結(jié)構(gòu)式
基本信息
中文別名
馬來(lái)酸哌西林馬來(lái)酸哌克昔林
肉堿棕櫚酰轉(zhuǎn)移酶1抑制劑(PERHEXILINE MALEATE)
英文別名
PexidWSM-3978
WSM 3978G
perhexilinemaleate
perhexilene maleate
rac Perhexiline Maleate
PERHEXILINE MALEATE SALT
PERHEXILINE MALEATE SALT USP/EP/BP
2-(2,2-dicyclohexylethyl)piperidinemaleate
2-(2,2-dicyclohexylethyl)-piperidinmaleate(1:1)
所屬類別
原料藥：防治心絞痛藥安全數(shù)據(jù)
WGK Germany2
WGK Germany2
RTECS號(hào)TM7068000
毒性LD50 in rats, mice (g/kg): >7, 4.37 orally (Causa, Perri)
常見(jiàn)問(wèn)題列表
生物活性
Perhexiline maleate 是一種有效的 carnitine palmitoyltransferase 1 (CPT1) 的抑制劑，對(duì)大鼠心臟CPT1和肝臟CPT1的IC50值分別為77 μM和148 μM。靶點(diǎn)
| Target | Value |
|
rat heart CPT1
(Cell-free assay) | 77 μM |
|
rat liver CPT1
(Cell-free assay) | 148 μM |
體外研究
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.
體內(nèi)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.