Perhexiline maleate 是一种具有口服活性的CPT1和CPT2抑制剂,可减少脂肪酸代谢。Perhexiline maleate 在肝细胞中诱导线粒体功能障碍和细胞凋亡 (apoptosis)。Perhexiline maleate 可穿过血脑屏障 (BBB),并显示出抗肿瘤活性。Perhexiline maleate 可用于癌症和心绞痛等心血管疾病的研究。
生物活性 | Perhexiline maleate is an orally activeCPT1andCPT2inhibitor that reduces fatty acid metabolism. Perhexiline maleate induces mitochondrial dysfunction andapoptosisin hepatic cells. Perhexiline maleate can cross the blood brain barrier (BBB) and shows anti-tumor activity. Perhexiline maleate can be used in the research of cancers, andcardiovascular diseaselike angina[1][2][5]. |
IC50& Target | IC50: 77 μM (Rat heart CPT 1), 148 μM (Rat liver CPT 1)[1] |
体外研究 (In Vitro) | Perhexiline (5-25 μM, 2-6 h) maleate reduces cell viability in HepG2 cells[2]. Perhexiline (5-25 μM, 2-6 h) maleate reduces cellular ATP content and Lactate dehydrogenase (LDH) release in HepG2 cells[2]. Perhexiline (20 μM, 2 h) maleate activates caspase 3/7 in HepG2 cells[2]. Perhexiline (5-25 μM, 4 h) maleate causes mitochondrial dysfunction in HepG2 cells[2]. Perhexiline (5 μM, 48 h) maleate selectively induces massive apoptosis in CLL cells (high expression of CPT)[3].
Cell Viability Assay[2] Cell Line: | HepG2 cells | Concentration: | 5, 10, 15, 25 μM | Incubation Time: | 2, 4, 6 h | Result: | Induced time- and concentration-dependent cytotoxicity in hepatic cells. |
Western Blot Analysis[2] Cell Line: | HepG2 cells | Concentration: | 5, 10, 15, 25 μM | Incubation Time: | 2 h | Result: | Reduced Bcl-2 and Mcl-1 level, and increased Bad level. |
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体内研究 (In Vivo) | Perhexiline (200 mg/kg, p.o., daily for 8 weeks) maleate reduces peripheral neural function in female DA rats[4]. Perhexiline (80 mg/kg, oral gavage, for 3 days) maleate demonstrates anti-tumor activity in glioblastoma mouse model[5].
Animal Model: | Orthotopic glioblastoma mouse model[5] | Dosage: | 80 mg/kg | Administration: | Oral gavage, for 3 days. | Result: | Reduces tumor size (MR imaging) and improves in overall survival. |
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中文名称 | 马来酸哌克昔林;马来酸双环己哌啶;马来酸环己哌啶;马来酸环基哌啶 |
运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
溶解性数据 | In Vitro: Ethanol : 20 mg/mL(50.82 mM;Need ultrasonic) DMSO : 3.57 mg/mL(9.07 mM;ultrasonic and warming and heat to 60℃) 配制储备液 1 mM | 2.5409 mL | 12.7045 mL | 25.4091 mL | 5 mM | 0.5082 mL | 2.5409 mL | 5.0818 mL | 10 mM | 0.2541 mL | 1.2705 mL | 2.5409 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用;
以下溶剂前显示的百 分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂: 10% EtOH 90% (20%SBE-β-CDin saline) Solubility: ≥ 2 mg/mL (5.08 mM); Clear solution
此方案可获得 ≥ 2 mg/mL (5.08 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 20.0 mg/mL 的澄清 EtOH 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。 2. 请依序添加每种溶剂: 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 0.5 mg/mL (1.27 mM); Clear solution
此方案可获得 ≥ 0.5 mg/mL (1.27 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 5.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。 3. 请依序添加每种溶剂: 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 0.5 mg/mL (1.27 mM); Clear solution
此方案可获得 ≥ 0.5 mg/mL (1.27 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 5.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。 4. 请依序添加每种溶剂: 10% DMSO 90%corn oil Solubility: ≥ 0.5 mg/mL (1.27 mM); Clear solution
此方案可获得 ≥ 0.5 mg/mL (1.27 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例,取 100 μL 5.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。 *以上所有助溶剂都可在本网站选购。
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