货号:A645812
同义名:
哌克昔林 马来酸盐
/ Perhexiline (maleate)
Perhexiline maleate是一种口服活性的 CPT1 和 CPT2 抑制剂,能够减少脂肪酸代谢,并在肝细胞中诱导线粒体功能障碍及细胞凋亡。它能穿过血脑屏障,展现出抗肿瘤活性,并可用于癌症和心绞痛等心血管疾病的研究。
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产品名称 | Transferase ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Tipifarnib |
+++
FTase, IC50: 0.6 nM |
99%+ | |||||||||||||||||
Tolcapone |
+
COMT, Ki: 30 nM |
99%+ | |||||||||||||||||
Lonafarnib |
+++
K-ras-4B, IC50: 2.8 nM H-ras, IC50: 1.9 nM |
99%+ | |||||||||||||||||
(E)-Daporinad |
++++
NMPRTase, Ki: 0.4 nM |
99%+ | |||||||||||||||||
FTI-277 HCl |
++++
FTase, IC50: 500 pM |
98% | |||||||||||||||||
A 922500 |
++
human DGAT-1, IC50: 7 nM mouse DGAT-1, IC50: 24 nM |
98% | |||||||||||||||||
Lomeguatrib |
++
O6-alkylguanine-DNA-alkyltransferas, IC50: 5 nM |
99%+ | |||||||||||||||||
PF-04620110 |
+
DGAT1, IC50: 19 nM |
99% | |||||||||||||||||
LB42708 |
+++
FTase (K-Ras), IC50: 0.8 nM FTase (N-ras), IC50: 1.2 nM |
98% | |||||||||||||||||
GGTI298 Trifluoroacetate | ✔ | 98%+ | |||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
描述 | Perhexiline maleate, an orally active inhibitor of CPT1 and CPT2, curtails fatty acid metabolism and induces mitochondrial dysfunction and apoptosis in hepatic cells. It can cross the blood-brain barrier (BBB) and exhibits anti-tumor properties. Perhexiline maleate is researched for its potential therapeutic applications in cancer and cardiovascular diseases such as angina[1].[2].[5]. |
体内研究 | In animal models, Perhexiline maleate (200 mg/kg, orally, daily for 8 weeks) impacts peripheral neural function in female DA rats[4] At 80 mg/kg via oral gavage for three days, it shows anti-tumor activity in a glioblastoma mouse model[5]. |
体外研究 | In studies involving HepG2 cells, Perhexiline maleate (5-25 μM, 2-6 h) diminishes cell viability. Perhexiline maleate also lowers cellular ATP content and increases Lactate dehydrogenase (LDH) release within the same concentration and time frame[2]. Additionally, at a concentration of 20 μM for 2 hours, it activates caspase 3/7, indicating apoptosis in HepG2 cells[2]. Furthermore, at a range of 5-25 μM over 4 hours, Perhexiline maleate leads to mitochondrial dysfunction in these cells[2]. When administered at 5 μM for 48 hours, it selectively triggers extensive apoptosis in CLL cells, which have high expression of CPT[3]. |
Concentration | Treated Time | Description | References | |
OVCAR-5/RFP | 4 µM | 10 days | To evaluate the killing effect of Perhexiline on ovarian cancer MRD cells, results showed that Perhexiline had a more pronounced killing effect on MRD cells in 3D microtumors than in 2D cultures. | Adv Healthc Mater. 2025 May;14(14):e2404072 |
OVCAR5 | 4 µM | 10 days | To evaluate the killing effect of Perhexiline on ovarian cancer MRD cells, results showed that Perhexiline had a more pronounced killing effect on MRD cells in 3D microtumors than in 2D cultures. | Adv Healthc Mater. 2025 May;14(14):e2404072 |
HepG2 cells | 10 µM | 24 hours | To investigate the effect of perhexiline on ApoA-I production, it was found that perhexiline significantly increased ApoA-I production | J Clin Invest. 2015 Oct 1;125(10):3819-30 |
Mouse pancreatic organoids (KPSC) | 4 µM | 48 hours | Inhibits growth and induces apoptosis in KPSC organoids | Cell Stem Cell. 2024 Jan 4;31(1):71-88. e8 |
Human PDAC organoids (WCM744 and WCM773) | 4 µM | 72 hours | Inhibits growth and induces apoptosis in human PDAC organoids | Cell Stem Cell. 2024 Jan 4;31(1):71-88. e8 |
Administration | Dosage | Frequency | Description | References | ||
Mice | Endotoxemia and sepsis models | Intragastric administration | 10 mg/kg | Once per 12 hours, twice | Perhexiline activated the expression of KLF14, significantly prolonged the survival rate of mice with LPS-induced endotoxemia and CLP-induced sepsis, and reduced lung tissue injury. | Cell Mol Immunol. 2022 Apr;19(4):504-515 |
Mice | High-fat diet-induced atherosclerosis model | Gavage | 10 mg/kg/d | 5 consecutive days | To evaluate the effect of perhexiline on HDL-C and ApoA-I levels, it was found that perhexiline significantly increased HDL-C and ApoA-I levels | J Clin Invest. 2015 Oct 1;125(10):3819-30 |
Nude mice | KPSC organoid xenograft model | Intraperitoneal injection | 16 mg/kg | Every other day for 4 weeks | Significantly inhibits the growth of KPSC xenografts | Cell Stem Cell. 2024 Jan 4;31(1):71-88. e8 |
NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
NCT02431221 | Hypertrophic Cardiomyopathy | Phase 3 | Withdrawn(Lack of efficacy in ... 展开 >>a preceding study.) 收起 << | - | - |
[1]E. Marc Jolicoeur, et al. 27 - Refractory Angina. Chronic Coronary Artery Disease, 2018, 412-431.
计算器 | ||||
存储液制备 | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
2.54mL 0.51mL 0.25mL |
12.70mL 2.54mL 1.27mL |
25.41mL 5.08mL 2.54mL |
CAS号 | 6724-53-4 |
分子式 | C23H39NO4 |
分子量 | 393.56 |
SMILES Code | O=C(O)/C=C/C(O)=O.C1(CC(C2CCCCC2)C3CCCCC3)NCCCC1 |
MDL No. | MFCD00057329 |
别名 | 哌克昔林 马来酸盐 ;Perhexiline (maleate) |
运输 | 蓝冰 |
存储条件 |
In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Inert atmosphere, 2-8°C |
溶解方案 |
DMSO: 3 mg/mL(7.62 mM),配合低频超声,并水浴加热至45℃助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO 无水乙醇: 25 mg/mL(63.52 mM),配合低频超声,并水浴加热至45℃助溶,注意:无水乙醇开封后,易挥发,也会吸收空气中的水分,导致溶解能力下降,请避免使用开封较久的乙醇
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