1. Neuronal Signaling Membrane Transporter/Ion Channel Epigenetics
  2. Monoamine Oxidase GABA Receptor Histone Demethylase
  3. Phenelzine sulfate

Phenelzine sulfate  (Synonyms: 硫酸苯乙肼; 苯肼,硫酸盐)

目录号: HY-B1018A 纯度: 99.92%
COA 产品使用指南 技术支持

Phenelzine sulfate 是一种抗抑郁剂,是一种不可逆的、具有口服活性的单胺氧化酶 (MAO-AMAO-B) 抑制剂。Phenelzine sulfate 可抑制 GABA 转氨酶和伯胺氧化酶 (PrAO),并螯合活性醛。Phenelzine sulfate 还能抑制 LSD1 (Ki 5.6 μM),并抑制氧化应激和脂肪生成。Phenelzine sulfate 可升高神经递质 (血清素、去甲肾上腺素、多巴胺) 的水平。Phenelzine sulfate 已被研究用于治疗神经系统、代谢和癌症疾病,例如抑郁症和焦虑症、中风、脊髓损伤、创伤性脑损伤、多发性硬化症、帕金森病、阿尔茨海默病、炎症性疼痛、肥胖症和前列腺癌。

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Phenelzine sulfate

Phenelzine sulfate Chemical Structure

CAS No. : 156-51-4

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥217
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10 mg ¥198
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25 mg ¥303
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50 mg ¥429
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100 mg ¥600
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500 mg ¥1650
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Other Forms of Phenelzine sulfate:

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Phenelzine sulfate, an antidepressant agent, is an irreversible and orally active monoamine oxidase (MAO-A and MAO-B) inhibitor. Phenelzine sulfate inhibits GABA transaminase and primary amine oxidase (PrAO), and sequester reactive aldehydes. Phenelzine sulfate also inhibits LSD1 (Ki: 5.6 μM) and suppresses oxidative stress and lipogenesis. Phenelzine sulfate elevates neurotransmitters (serotonin, norepinephrine, dopamine). Phenelzine sulfate is studied in neurological, metabolic and cancer diseases for depression and anxiety disorders, stroke, spinal cord injury, traumatic brain injury, multiple sclerosis, Parkinson’s disease, Alzheimer’s disease, inflammatory pain, obesity and prostate cancer[1][2][3][4].

体外研究
(In Vitro)

Phenelzine sulfate 可抑制重组小鼠 MAOA/MAOB、PIPOX、PCYOX1、ALDH2 和 SCRN3 蛋白[2]
Phenelzine (80 μM; 48 h; H460) sulfate 在 [3H] 胸苷掺入实验中,对 H460 细胞增殖的抑制率低于 50%[3]
Phenelzine (10-100 μM;24 小时;大鼠视网膜神经节细胞) sulfate 可减少 3-Aminopropanal 引起的毒性[1]
Phenelzine (150-300 nmol;30分钟;磷酸盐缓冲液) sulfate 可降低体外丙烯醛水平[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cytotoxicity Assay[1]

Cell Line: Rat retinal ganglion cells
Concentration: 10 μM, 20 μM, 30 μM, 40 μM, 50 μM, 100 μM
Incubation Time: 24 h
Result: LDH release was measured 24 hours after cotreatment with 3-Aminopropanal, showing reduced toxicity.

Western Blot Analysis[3]

Cell Line: LNCaP
Concentration: 3 μM, 10 μM, 20 μM, 40 μM
Incubation Time: 48 h
Result: No significant changes in H3K4Me2 or total H3 levels were observed.

Cell Proliferation Assay[3]

Cell Line: H460
Concentration: 80 μM
Incubation Time: 48 h
Result: Less than 50% reduction in 3H-thymidine incorporation.
体内研究
(In Vivo)

Phenelzine (31.6 mg/kg (0.028%);饮用;每日一次;12 周) sulfate 表现出比对照组更低的体脂含量、皮下白色脂肪组织 (WAT) 质量和骨骼肌脂质含量,且不降低体重增长或食物消耗[4]
Phenelzine (15 mg/kg;腹腔注射,损伤后 15 分钟) sulfate 可降低大鼠脊髓损伤 (SCI) 模型中的丙烯醛和 4-HNE 水平,并促进恢复[1]。Phenelzine sulfate (水族箱水) 可通过降低氧化应激和维持多巴胺水平来减轻百草枯诱导的斑马鱼神经毒性,并促进斑马鱼脊髓损伤模型中的轴突再生和髓鞘再生[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female C57BL/6 micEAE was induced in female C57/BL mice with MOG35-55 (HY-P1240)(subcutaneous injection).[5]
Dosage: 15 mg/kg
Administration: IP; daily, for 28 days
Result: Reduced disease severity in the chronic phase and was associated with substantial improvements in exploratory behavior.
Showed a normalization of 5-HT levels in the ventral horn of the spinal cord that might account for the improvements in behavioral outcomes.
Animal Model: Rats; traumatic brain injury (TBI) model, induced by controlled cortical impact (CCI-TBI)[1]
Dosage: 15 mg/kg
Administration: IP; once; 15 minutes post-injury
Result: Prevented the decrease in respiratory control ratio, increased cortical tissue sparing from 86 to 97%, and reduced 4-HNE levels in mitochondria.
Animal Model: Gerbils (male, 8 weeks); global ischemia model, induced by carotid ligation for 5 minutes followed by reperfusion[1]
Dosage: 15 mg/kg, 30 mg/kg
Administration: IP; once daily; 6 days
Result: Significantly attenuated neuronal loss in the hippocampal CA1 region compared to ischemia-vehicle gerbils.
Animal Model: C57BL/6 mice (male, 9 weeks); no disease model[4]
Dosage: 31.6 mg/kg
Administration: Drinking water; once daily; 12 weeks
Result: Exhibited lower body fat content, subcutaneous WAT mass and lipid content in skeletal muscles than control, without decreased body weight gain or food consumption. Phenelzine impaired the lipogenic but not the antilipolytic actions of insulin in WAT.
Lowered MAO activity and hydrogen peroxide release in WAT.
Decreased phosphoenolpyruvate carboxykinase (PEPCK) expression in subcutaneous WAT.
Animal Model: C57BL/6 mice (male, 9 weeks); no disease model[4]
Dosage: 31.6 mg/kg
Administration: Drinking water; once daily; 12 weeks
Result: Lowered non-fasting blood glucose levels.
Clinical Trial
分子量

234.27

Formula

C8H14N2O4S

CAS 号
性状

固体

颜色

White to off-white

中文名称

硫酸苯乙肼

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
细胞实验: 

DMSO 中的溶解度 : ≥ 100 mg/mL (426.86 mM; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 4.2686 mL 21.3429 mL 42.6858 mL
5 mM 0.8537 mL 4.2686 mL 8.5372 mL
查看完整储备液配制表

* 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。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物实验:

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

  • 方案 一

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (8.88 mM); 澄清溶液

    此方案可获得 ≥ 2.08 mg/mL(饱和度未知)的澄清溶液。

    1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL

    生理盐水的配制:将 0.9 g 氯化钠,溶解于 ddH₂O 并定容至 100 mL,可以得到澄清透明的生理盐水溶液。
  • 方案 二

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.08 mg/mL (8.88 mM); 澄清溶液

    此方案可获得 ≥ 2.08 mg/mL(饱和度未知)的澄清溶液。

    1 mL 工作液为例,取 100 μL 20.8 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。

    2 g SBE-β-CD(磺丁基醚 β-环糊精)粉末定容于 10 mL 的生理盐水中,完全溶解至澄清透明。
动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
请输入您的动物体内配方组成:
%
DMSO +
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括:DMSO ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。

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

您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
连续给药周期超过半月以上,请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
纯度 & 产品资料

纯度: 99.96%

参考文献

完整储备液配制表

* 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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 4.2686 mL 21.3429 mL 42.6858 mL 106.7145 mL
5 mM 0.8537 mL 4.2686 mL 8.5372 mL 21.3429 mL
10 mM 0.4269 mL 2.1343 mL 4.2686 mL 10.6714 mL
15 mM 0.2846 mL 1.4229 mL 2.8457 mL 7.1143 mL
20 mM 0.2134 mL 1.0671 mL 2.1343 mL 5.3357 mL
25 mM 0.1707 mL 0.8537 mL 1.7074 mL 4.2686 mL
30 mM 0.1423 mL 0.7114 mL 1.4229 mL 3.5571 mL
40 mM 0.1067 mL 0.5336 mL 1.0671 mL 2.6679 mL
50 mM 0.0854 mL 0.4269 mL 0.8537 mL 2.1343 mL
60 mM 0.0711 mL 0.3557 mL 0.7114 mL 1.7786 mL
80 mM 0.0534 mL 0.2668 mL 0.5336 mL 1.3339 mL
100 mM 0.0427 mL 0.2134 mL 0.4269 mL 1.0671 mL
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