Perphenazine 是一种具有口服活性的多巴胺受体 (dopamine receptor) 和组胺-1 受体 (histamine-1 receptor) 拮抗剂,Ki值分别为 0.56 nM (D2)、0.43 nM (D3)、0.6 nM (5-HT2A)。Perphenazine 还可与 Alpha-1A 肾上腺素受体 (Alpha-1A adrenergic receptor) 结合。Perphenazine 抑制癌细胞增殖，并诱导细胞凋亡。Perphenazine 可用于精神疾病、癌症、炎症的研究。
| 生物活性 | Perphenazine is an orally activedopamine receptorandhistamine-1 receptorantagonist, withKivalues of 0.56 nM (D2), 0.43 nM (D3), 6 nM (5-HT2A), respectively. Perphenazine also binds toAlpha-1Aadrenergic receptor. Perphenazine inhibitscancercell proliferation, and inducesapoptosis. Perphenazine can be used in the research of mental disease,cancer, inflammation[1][3][5]. |
| IC50& Target[1] | D2Receptor 0.56 nM (Ki) | D3Receptor 0.43 nM (Ki) | D4Receptor 28.5 nM (Ki) | 5-HT2AReceptor 5.6 nM (Ki) | 5-HT6Receptor 17 nM (Ki) | 5-HT7Receptor 23 nM (Ki) | H2Receptor 132 nM (Ki) | 5-HT1AReceptor 421 nM (Ki) |
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体外研究
(In Vitro) | Perphenazine (40 μM, 48 h) inhibits cell viability, and induces cell apoptosis mediated by CTSD (Cathepsin D) in L02 cells[2].
Perphenazine (30 μM, 24 h) induces intense lysosome vacuolation, impaired lysosomal membrane, and induces lysosomal membrane permeabilization (LMP), ultimately triggering lysosomal cell death in L02 cells[2].
Perphenazine (10-40 μM, 24 h) inhibits autophagic flux in L02 cells[2].
Perphenazine (1 μM, 24 h) decreases glioblastoma U-87 MG cell migration and invasion[4].
Cell Viability Assay[2] | Cell Line: | L02 cells | | Concentration: | 10-100 μM | | Incubation Time: | 12, 24, 48 h | | Result: | Inhibited cell viability in a concentration and time-dependent manner. |
Western Blot Analysis[2] | Cell Line: | L02 cells | | Concentration: | 10, 20, 30, and 40 μM | | Incubation Time: | 24 h | | Result: | Increased LC3 I/II and P62/SQSTM1 levels |
Cell Migration Assay[4] | Cell Line: | U-87 MG cells | | Concentration: | 1 μM | | Incubation Time: | 0, 3, 6, 9, 12, and 24 h | | Result: | Increased the wound closure in human glioblastoma cell cultures from 24.6 to 62.7%. |
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体内研究
(In Vivo) | Perphenazine (oral gavage, 180 mg/kg, every other day for 21 days) induces liver injury and lysosomal membrane damage in ICR mice[2].
Perphenazine (oral administration, 10 mg/kg, every other day for 6 days) attenuates morphological phenotype in mouse models of Th2-type allergic dermatitis[3].
| Animal Model: | ICR mice[2] | | Dosage: | 10, 30, 60, 120, 180 mg/kg | | Administration: | Oral gavage, every other day for 21 days. | | Result: | Increased histological injury and aminotransferases compared with control. |
| Animal Model: | Oxazolone-treated animal model of dermatitis[3] | | Dosage: | 10 mg/kg | | Administration: | Oral administration, every other day for 6 days | | Result: | Decreased The levels of mice ear swelling. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | 4°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light) |
| 溶解性数据 | In Vitro: DMSO : 100 mg/mL(247.54 mM;Need ultrasonic) H2O :< 0.1 mg/mL(insoluble) 配制储备液 | 1 mM | 2.4754 mL | 12.3772 mL | 24.7543 mL | | 5 mM | 0.4951 mL | 2.4754 mL | 4.9509 mL | | 10 mM | 0.2475 mL | 1.2377 mL | 2.4754 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 (protect from light)。-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% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (6.19 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (6.19 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 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。 2. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: 2.5 mg/mL (6.19 mM); Suspended solution; Need ultrasonic
此方案可获得 2.5 mg/mL (6.19 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。 以 1 mL 工作液为例，取 100 μL 25.0 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。 3. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (6.19 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (6.19 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 25.0 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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