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马来酸哌克昔林

马来酸哌克昔林用途

Perhexiline maleate是有效的肉碱棕榈酰转移酶1 (carnitine palmitoyltransferase 1) 抑制剂,对大鼠心脏和肝脏CPT 1的 IC50 值分别为77 和 148 μM。

马来酸哌克昔林名称

[ CAS 号 ]:
6724-53-4

[ 中文名 ]:
马来酸哌克昔林

[ 英文名 ]:
Perhexiline maleate

[英文别名 ]:

perhexilline maleate
Perhexiline maleate (USAN)
EINECS 229-775-5
Pexid
2-(2,2-Dicyclohexylethyl)piperidine maleate
DSSTox_CID_1114
perhexilene maleate
Perhexiline maleate

马来酸哌克昔林生物活性

[ 描述 ]:

Perhexiline maleate是有效的肉碱棕榈酰转移酶1 (carnitine palmitoyltransferase 1) 抑制剂,对大鼠心脏和肝脏CPT 1的 IC50 值分别为77 和 148 μM。

[ 相关类别 ]:

信号通路 >> 其他 >> 其他

研究领域 >> 癌症

研究领域 >> 心血管疾病

[ 靶点 ]

IC50: 77 μM (Rat heart CPT 1), 148 μM (Rat liver CPT 1)[1]

[体外研究]

在用0.01和1μM的哌可昔林处理24,48和72小时后,SH-SY5Y细胞中的NDM29ncRNA表达水平逐渐增加,在处理48小时后达到峰值。哌克昔林治疗增加了NB细胞对抗生素治疗的敏感性。马来酸哌可昔林的共同施用增强了顺铂降低NB细胞的体外克隆形成潜力的功效[2]。

[体内研究]

与用DMSO处理的小鼠相比,哌可昔林和顺铂的共同施用产生抗肿瘤效果的明显增强,导致显着改善的无进展存活。哌可昔林有利于NB细胞向分化表型转变[2]。

[细胞实验]

使用MTT测定评估抗肿瘤药物对神经母细胞瘤细胞存活的影响。铺板后约24小时，将细胞在37℃下暴露于马来酸哌可昔林（0.01μM）48小时。细胞毒性表示为相对于未处理细胞存活的细胞百分比[2]。

[动物实验]

小鼠：在方案a中，将21只小鼠分成4组：对照载体组：DMSO;顺铂（3 mg / kg /剂量）治疗组;哌克昔林（1 mg / kg /剂量）治疗组和;哌克昔林（1mg / kg /剂）和顺铂（3mg / kg /剂）治疗组。在方案b中，将20只小鼠分成4组：对照载体组：DMSO;哌克昔林（3 mg / kg /剂量）治疗组;顺铂（5 mg / kg /剂量）治疗组;哌克昔林（3 mg / kg /剂量）和顺铂（5 mg / kg /剂量）治疗组[2]。

[参考文献]

[1]. Kennedy JA, et al. Inhibition of carnitine palmitoyltransferase-1 in rat heart and liver by Perhexiline and amiodarone. Biochem Pharmacol. 1996 Jul 26;52(2):273-80.

[2]. Vella S, et al. Perhexiline maleate enhances antitumor efficacy of cisplatin in neuroblastoma by inducing over-expression of NDM29 ncRNA. Sci Rep. 2015 Dec 17;5:18144.

[相关活性小分子]

马来酸哌克昔林物理化学性质

[ 沸点 ]:
574.1ºC at 760 mmHg

[ 熔点 ]:
181-183ºC

[ 分子式 ]:
C₂₃H₃₉NO₄

[ 分子量 ]:
393.56000

[ 闪点 ]:
301ºC

[ 精确质量 ]:
393.28800

[ PSA ]:
86.63000

[ LogP ]:
5.33600

[ 外观性状 ]:
white to tan

[ 储存条件 ]:
-20?C Freezer, Under Inert Atmosphere

[ 水溶解性 ]:
DMSO: ≥5mg/mL

马来酸哌克昔林MSDS

详细MSDS(安全技术说明书)

马来酸哌克昔林毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: TM7068000

CAS REGISTRY NUMBER :: 6724-53-4

LAST UPDATED :: 199410

DATA ITEMS CITED :: 9

MOLECULAR FORMULA :: C19-H35-N.C4-H4-O4

MOLECULAR WEIGHT :: 393.63

WISWESSER LINE NOTATION :: T6MTJ B1Y- AL6TJ&- AL6TJ &QV1U1VQ -C

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 636 mg/kg/89D-I

TOXIC EFFECTS :: Liver - jaundice, other or unclassified Skin and Appendages - dermatitis, other (after systemic exposure)

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 4693 mg/kg/3Y

TOXIC EFFECTS :: Behavioral - muscle weakness Liver - hepatitis, fibrous (cirrhosis, post-necrotic scarring)

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 2150 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Behavioral - ataxia Nutritional and Gross Metabolic - weight loss or decreased weight gain

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 106 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Lungs, Thorax, or Respiration - respiratory depression Nutritional and Gross Metabolic - body temperature decrease

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >2 gm/kg

TOXIC EFFECTS :: Skin and Appendages - dermatitis, other (after systemic exposure) Skin and Appendages - hair

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 2641 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Behavioral - ataxia Nutritional and Gross Metabolic - weight loss or decreased weight gain

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 107 mg/kg

TOXIC EFFECTS :: Behavioral - ataxia Lungs, Thorax, or Respiration - respiratory depression Nutritional and Gross Metabolic - body temperature decrease

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >2 gm/kg

TOXIC EFFECTS :: Skin and Appendages - dermatitis, other (after systemic exposure) Skin and Appendages - hair

MUTATION DATA

TYPE OF TEST :: Mutation in microorganisms

TEST SYSTEM :: Rodent - hamster Lung

DOSE/DURATION :: 10 umol/L

REFERENCE :: MUREAV Mutation Research. (Elsevier Science Pub. B.V., POB 211, 1000 AE Amsterdam, Netherlands) V.1- 1964- Volume(issue)/page/year: 157,1,1985

马来酸哌克昔林安全信息

[ 危险品运输编码 ]:
NONH for all modes of transport

[ WGK德国 ]:
2

[ RTECS号 ]:
TM7068000

[ 海关编码 ]:
2933399090

马来酸哌克昔林合成路线

详细合成路线

马来酸哌克昔林上下游产品

马来酸哌克昔林上游产品

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马来酸哌克昔林海关

[ 海关编码 ]: 2933399090

[ 中文概述 ]:
2933399090. 其他结构含非稠合吡啶环的化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:20.0%

[ 申报要素 ]: 品名, 成分含量, 用途, 乌洛托品请注明外观, 6－己内酰胺请注明外观, 签约日期

[ Summary ]:
2933399090. other compounds containing an unfused pyridine ring (whether or not hydrogenated) in the structure. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

马来酸哌克昔林文献

Torsade de pointes associated with perhexiline maleate therapy.

Aust. N. Z. J. Med. 20(6) , 818-20, (1990)

Multiform ventricular tachycardia (torsade de pointes) is a recognised proarrhythmic effect of drugs which prolong the QT interval. A case is now described for the first time where torsade de pointes ...

Further studies on the pharmacokinetics of perhexiline maleate in humans.

Xenobiotica 16(1) , 63-8, (1986)

We have performed single-dose pharmacokinetic studies on perhexiline in eight young volunteers, each given 300 mg of Pexid orally, using an h.p.l.c. method for the separation and quantification of the...

Stimulatory effect of perhexiline maleate on the basal and LHRH-stimulated luteinizing hormone release from rat pituitary cell aggregates in vitro.

Res. Commun. Mol. Pathol. Pharmacol. 87(2) , 115-23, (1995)

Perhexiline maleate (PM) is an anti-anginal agent of amphiphilic character involved in lipidosis disorders. Experiments were carried out to study PM action on LH release from rat anterior pituitary ce...

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