2. 诱导疾病模型产品 Membrane Transporter/Ion Channel Autophagy
  3. 免疫与炎症疾病模型 神经系统疾病模型 消化系统疾病模型 Monoamine Transporter Autophagy
  4. 胃肠炎症及溃疡模型 帕金森综合症模型 胃肠道疾病模型
  5. 胃溃疡模型
  6. Reserpine

Reserpine  (Synonyms: 利血平)

目录号: HY-N0480 纯度: 98.37%
COA 产品使用指南

摩尔计算器

Reserpine 是囊泡单胺转运蛋白 2 (VMAT2) 的抑制剂。

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Reserpine Chemical Structure

Reserpine Chemical Structure

CAS No. : 50-55-5

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥550
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100 mg ￥500
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Customer Review

Other Forms of Reserpine:

Reserpine 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

Reserpine is an inhibitor of the vesicular monoamine transporter 2 (VMAT2).

IC50 & Target

VMAT2[1]
细胞效力
(Cellular Effect)
Cell Line Type Value Description References
HEK293 IC50
15.5 nM
Compound: 5770
Substrate uptake and inhibition of the Vesicular Amine Transporter 2 (VMAT2, SLC18A2) as assessed by uptake of a fluorescent substrate (FFN206) in HEK-293 JumpIN-SLC18A2 cells
Substrate uptake and inhibition of the Vesicular Amine Transporter 2 (VMAT2, SLC18A2) as assessed by uptake of a fluorescent substrate (FFN206) in HEK-293 JumpIN-SLC18A2 cells
10.5281/zenodo.7360403
HEK293 IC50
50 nM
Compound: 5770
Substrate uptake and inhibition of the chromaffin granule amine transporter (VAT1, VMAT1, SLC18A1) as assessed by uptake of a fluorescent substrate (FFN206) in HEK-293 JumpIN-SLC18A1 cells
Substrate uptake and inhibition of the chromaffin granule amine transporter (VAT1, VMAT1, SLC18A1) as assessed by uptake of a fluorescent substrate (FFN206) in HEK-293 JumpIN-SLC18A1 cells
10.5281/zenodo.7360413
HEp-2 ED50
> 20 μg/mL
Compound: Reserpin
Cytotoxicity against human Hep2 cells after 72 hrs
Cytotoxicity against human Hep2 cells after 72 hrs
[PMID: 18500841]
HL-60 IC50
67 μM
Compound: 8
Cytotoxicity against human HL60 cells by MTT assay
Cytotoxicity against human HL60 cells by MTT assay
[PMID: 15974606]
MCF7 IC50
0.003 μg/mL
Compound: Reserpine
Cytotoxicity against vinblastin-sensitive human MCF7 cells assessed as growth inhibition after 72 hrs by SRB assay
Cytotoxicity against vinblastin-sensitive human MCF7 cells assessed as growth inhibition after 72 hrs by SRB assay
[PMID: 25536852]
MCF7 IC50
0.037 μg/mL
Compound: Reserpine
Cytotoxicity against human MCF7 cells assessed as growth inhibition after 72 hrs by SRB assay
Cytotoxicity against human MCF7 cells assessed as growth inhibition after 72 hrs by SRB assay
[PMID: 25536852]
MCF7 IC50
0.31 μg/mL
Compound: Reserpine
Cytotoxicity against human MCF7 cells assessed as growth inhibition after 72 hrs by SRB assay in presence of vinblastine
Cytotoxicity against human MCF7 cells assessed as growth inhibition after 72 hrs by SRB assay in presence of vinblastine
[PMID: 25536852]
MRC5 GI50
14.7 μM
Compound: Reserpine
Cytotoxicity against human MRC5 cells assessed as reduction in cell viability after 72 hrs by MTT assay
Cytotoxicity against human MRC5 cells assessed as reduction in cell viability after 72 hrs by MTT assay
[PMID: 29597171]
Vero C1008 CC50
25 μM
Compound: 70
Cytotoxicity against African green monkey Vero E6 cells incubated for 2 days by the MTS assay
Cytotoxicity against African green monkey Vero E6 cells incubated for 2 days by the MTS assay
[PMID: 32845145]
体外研究
(In Vitro)

Reserpine is an inhibitor of the vesicular monoamine transporter 2 (VMAT2). Reserpine displays a significant effect on the density of dopamine D1 receptors (F2,12=8.81, p<0.01) in the rat striatum. The affinity (Kd) for the dopamine D1 and D2 receptors during withdrawal from acute and chronic administration of reserpine is not change[1]. IC50 values of 43.9 and 54.9 μM are obtained after 1 day of treatment with Reserpine in JB6 P+ and HepG2-C8 cells, respectively. Reserpine induces luciferase activity in a dose-dependent manner at concentrations ranging from 5 to 50 μM, and no significant induction is observed at concentrations lower than 5 μM. Results demonstrate that Reserpine (2.5 to 10 μM) also increases the protein expression of Nrf2, HO-1, and NQO1. Reserpine at concentrations of 2.5 to 10 μM decreases the mRNA expression of DNMT1, DNMT3a, and DNMT3b in a concentration-dependent manner in JB6 P+ cells after 7 days of treatment. Reserpine at 10 μM generates a significant difference for DNMT3a expression (p<0.05)[2].

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

Reserpine 相关抗体:
体内研究
(In Vivo)

Reserpine 可用于动物建模，以构建胃肠道溃疡和抑郁症模型，从慢性 (14 天) 而非急性利血平中停药（48 小时）可显著减少大鼠的不动时间（F2,18=3.68，p<0.05），但增加攀爬时间（F2,18=4.48，p<0.02），并且不会改变大鼠强迫游泳试验 (FST) 中的游泳时间 (F2,18=1.78；NS)，与对照动物相比，剂量为 5 mg/kg 体重的 Reserpine 可显著增加香草扁桃酸 (VMA) 的尿液排泄情况。接受 Reserpine 治疗的动物体内排出的 5-羟基吲哚乙酸 (5-HIAA) 量比对照组多。Reserpine 治疗后观察到剂量依赖性低血压。与对照组相比，剂量为 0.5、1、5、10 和 15 μg/kg 的 Reserpine 可显著 (p<0.01) 降低血压[1][3]。

诱导胃溃疡[4][5][6]
致病原理
外周胆碱能和肾上腺素能机制参与利血平引起的溃疡。α-肾上腺素受体拮抗剂 (phenoxybenzamine (HY-B0431) and phentolamine (HY-12717))可显着降低利血平的溃疡形成活性，但 β-肾上腺素受体阻滞剂 propranolol (HY-B0573B) 则不会显着降低利血平的溃疡活性[6]。
具体造模方法：
大鼠：Wistar 大鼠 • 雄性 • 200-290 g[4]
给药方式：5 mg/kg • 腹腔注射 • 注射 18 h 后处死大鼠
小鼠：ICR 小鼠 • 雄性 • 7 周龄[5]
给药方式：10 mg/kg • 腹腔注射 • 每天一次，共 3 天
Note
(1)溶解于柠檬酸盐缓冲液和5%盐水中，每周三次，通过灌胃途径，持续16周。 (2)通过特异性生化标志物如血清胃泌素水平、TBARS和谷胱甘肽来确定癌症诱导水平，然后在8周和16周的两个时间段进行组织病理学分析。
造模成功指标
个体表型变化：引起明显的胃腺溃疡，并引起胃粘膜溶酶体释放游离的β-葡萄糖醛酸酶。
分子变化：利血平诱导的胃溃疡对照小鼠胃分泌量增加，pH值（1.04）降低，血清IL-6、IL-12、TNF-α和IFN-γ增加。
相关产品： /
拮抗产品： /

诱导抑郁症[7][8]
致病原理
利血平是囊泡单胺转运蛋白 2 的不可逆抑制剂，可调节单胺在突触囊泡中的积累及其从突触的再摄取。因此，利血平会抑制单胺突触前的再摄取和储存，导致单胺耗竭和抑郁症[7]。
具体造模方法：
大鼠：Wistar 大鼠 • 雄性 • 120-150 g[7]
给药方式：0.5 mg/kg • 腹腔注射 • 每天一次，共 14 天
小鼠：C57BL/6 小鼠 • 雄性 • 7 周龄[8]
给药方式：0.5 mg/kg • 腹腔注射 • 每天一次，共 10 天
Note
(1)将利血平用冰醋酸稀释至蒸馏水中醋酸的最终浓度为0.5%。
造模成功指标
个体表型变化：活动笼内自发运动能力显着下降，不动潜伏期缩短，强迫游泳试验（FST）中不动持续时间增加，表明运动障碍和抑郁加重 表型。
分子变化：利血平给药显着增加皮质MDA（丙二醛）含量，减少GSH（谷胱甘肽），增加TNF-ɑ和减少BDNF（脑源性神经营养因子）。 皮质去甲肾上腺素 (NE)、血清素 (5-HT) 和多巴胺 (DA) 显着下降
相关产品： /
拮抗产品： /

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

608.68

Formula

C33H40N2O9
CAS 号
性状

固体

颜色

White to light yellow

中文名称

利血平；蛇根草素；蛇根碱；血安平；阿达芬；安达血平；降压静；利舍平
结构分类
初始来源
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
细胞实验： 

DMSO 中的溶解度 : 25 mg/mL (41.07 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.6429 mL 8.2145 mL 16.4290 mL
5 mM 0.3286 mL 1.6429 mL 3.2858 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 (protect from light)。-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: ≥ 2.5 mg/mL (4.11 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL（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；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% Corn Oil

    Solubility: ≥ 2.5 mg/mL (4.11 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。

    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。

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

只
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 (protect from light)

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: 99.83%

COA (288 KB) HNMR (200 KB) LCMS (291 KB)

产品使用指南 (1538 KB)
参考文献
Kinase Assay
[2]

After incubation for 24 h, JB6 P+ cells (1×105 cells/10-cm dish) are treated with various concentrations of Reserpine. Whole cell lysates are prepared from the treated cells using radioimmunoprecipitation assay buffer supplemented with a protease inhibitor cocktail, and a BCA kit is used to determine protein concentrations[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay
[2]

JB6 P+ cells are seeded in 96-well plates containing Minimum essential media (MEM) at a density of 1×104 cells/mL (100 μL/well) for 1, 3, and 5 days, and HepG2-C8 cells are seeded in plates containing DMEM. After incubation for 24 h, the cells are treated with either DMSO or various concentrations of Reserpine. For JB6 P+ cells, the medium is changed every 2 days for the 3-day and 5-day treatments. Cell viability is assessed using a MTS assay kit according to the manufacturer’s instructions. The absorbance of the formazan product is read at 490 nm, and the cell viability is calculated and compared with the DMSO control group[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[3]

Albino rats of either sex weighing between 100 to 150 g are used in the study. They are acclimatized to the laboratory conditions for at least 10 days prior to the experiment and provided with standard diet and water ad libitum with 12 h light and dark cycle. Animals are divided into different groups of six each and are housed individually in metabolic cages. Group 1: Control animals treated with DMSO intraperitoneally at a dose of 0.1 mL/100 g body weight. Group 2: Animals administered intraperitoneally with Reserpine at a dose of 5 mg/kg body weight. The 24 h urine samples from the point of drug administration are collected for each animal[3].

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

Reserpine 相关分类

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 (protect from light)。-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 1.6429 mL 8.2145 mL 16.4290 mL 41.0725 mL
5 mM 0.3286 mL 1.6429 mL 3.2858 mL 8.2145 mL
10 mM 0.1643 mL 0.8214 mL 1.6429 mL 4.1072 mL
15 mM 0.1095 mL 0.5476 mL 1.0953 mL 2.7382 mL
20 mM 0.0821 mL 0.4107 mL 0.8214 mL 2.0536 mL
25 mM 0.0657 mL 0.3286 mL 0.6572 mL 1.6429 mL
30 mM 0.0548 mL 0.2738 mL 0.5476 mL 1.3691 mL
40 mM 0.0411 mL 0.2054 mL 0.4107 mL 1.0268 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Reserpine50-55-5利血平蛇根草素蛇根碱血安平阿达芬安达血平降压静利舍平Monoamine TransporterAutophagyInhibitorinhibitorinhibit

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