Perhexiline maleate is a potent carnitine palmitoyltransferase 1 (CPT 1) inhibitor with IC₅₀s of 77 and 148 μM for rat heart and liver CPT 1, respectively.

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

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^[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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^[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

393.56

C₂₃H₃₉NO₄

6724-53-4

马来酸哌克昔林

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Ethanol : 20 mg/mL (50.82 mM; Need ultrasonic)

DMSO : 5 mg/mL (12.70 mM; Need ultrasonic)

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°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

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-CD in 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 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

  将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
• 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。

  将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

• 3.

  请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in 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 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

  将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
• 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。

• [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.

The effect of antitumoral drugs on neuroblastoma cell survival is evaluated using the MTT assay. Approximately 24 hours after plating, cells are exposed to Perhexiline maleate (0.01 μM) for 48 hours at 37°C. Cytotoxicity is expressed as the percentage of cells surviving in relation to untreated cells^[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Mice: In protocol a, 21 mice are divided in 4 groups: control vehicle group: DMSO; cisplatin (3 mg/kg/dose) treated group; Perhexiline (1 mg/kg/dose) treated group and; Perhexiline (1 mg/kg/dose) and cisplatin (3 mg/kg/dose) treated group. In protocol b, 20 mice are divided in 4 groups: control vehicle group: DMSO; Perhexiline (3 mg/kg/dose) treated group; cisplatin (5 mg/kg/dose) treated group; Perhexiline (3 mg/kg/dose) and cisplatin (5 mg/kg/dose) treated group^[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

• [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.