1. Neuronal Signaling
  2. Serotonin Transporter Dopamine Transporter
  3. Bupropion hydrochloride

Bupropion hydrochloride  (Synonyms: 盐酸氨非他酮; Amfebutamone hydrochloride)

目录号: HY-B0403A 纯度: 99.94%
COA 产品使用指南

Bupropion (Amfebutamone) hydrochloride 是一种口服有效,选择性的 5-羟色胺再摄取抑制剂 (SSRI)。Bupropion hydrochloride 阻断多巴胺 (DA) 摄取或 Methamphetamine 诱导的 DA 释放,IC50 分别为 1.76 μM 和 14.2 μM。Bupropion hydrochloride 是一种非典型氨基酮类抗抑郁剂,可用于辅助戒烟的研究。

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Bupropion hydrochloride Chemical Structure

Bupropion hydrochloride Chemical Structure

CAS No. : 31677-93-7

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10 mM * 1 mL in DMSO ¥613
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50 mg ¥558
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100 mg ¥930
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Other Forms of Bupropion hydrochloride:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Bupropion (Amfebutamone) hydrochloride is an orally active, selective serotonin reuptake inhibitor (SSRI).Bupropion block dopamine (DA) uptake or Methamphetamine-induced DA release with IC50s of 1.76 μM and 14.2 μM, respectively. Bupropion hydrochloride is an atypical antidepressant of the aminoketone group. Bupropion hydrochloride can be used for the research of smoking cessation aid[1][2][3].

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
HEK293 IC50
12.6 μM
Compound: Bupropion
Inhibition of the Norepinephrine transporter (NET, SLC6A2) as assessed by GPCR-mediated changes in cell morphology using the impedance-based transporter activity through receptor activation (TRACT) assay in HEK-293 JumpIN-SLC6A2 cells
Inhibition of the Norepinephrine transporter (NET, SLC6A2) as assessed by GPCR-mediated changes in cell morphology using the impedance-based transporter activity through receptor activation (TRACT) assay in HEK-293 JumpIN-SLC6A2 cells
[PMID: 34112854]
体外研究
(In Vitro)

Bupropion (Amfebutamone) hydrochloride inhibits CYP2D6 with the IC50 of 58 μM[1].
Bupropion hydrochloride, an atypical antidepressant, induces endoplasmic reticulum stress and caspase-dependent cytotoxicity in SH-SY5Y cells[3].
Bupropion hydrochloride activates caspase 3 through the induction of endoplasmic reticulum stress responses and activation of JNK, and consequently induces apoptotic cell death in SH-SY5Y cells[3].
Bupropion (1-100 μg/mL) hydrochloride reduces cell viability. Bupropion-induced reduction in cell viability may have been a consequence of apoptotic mechanisms[3].
Bupropion (100 μg/mL) hydrochloride increases the phosphorylated forms of EIF-2α, JNK, and p38 MAPK, and the expression of GRP78 within 1 h[3].

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

Cell Viability Assay[3]

Cell Line: SH-SY5Y human catecholaminergic cells
Concentration: 0, 1, 10, 50, and 100 µg/mL
Incubation Time: 24 hours
Result: Cell viability decreased significantly in a concentration-dependent manner.

Western Blot Analysis[3]

Cell Line: SH-SY5Y human catecholaminergic cells
Concentration: 100 μg/mL
Incubation Time: 1, 3, 8, 24 hours
Result: The immunoreactivity for p-EIF-2α increased significantly within 1 h of Bupropion treatment and was sustained for 3 h, indicating that Bupropion rapidly stimulates PERK.
Slightly but significantly increased the expression of GRP78 and markedly activated JNK. This early activation of the ER stress pathways by Bupropion returned to basal levels 8 h after treatment.
体内研究
(In Vivo)

Bupropion (Amfebutamone) hydrochloride shows convulsant and anticonvulsant effects in mice. Bupropion dose-dependently causes clonic convulsions in mice, with the CD50 (convulsive dose50, i.e., the dose producing convulsions in 50% of mice) at 119.7 mg/kg[4].
Bupropion (10, 15, 20 and 40 mg/kg., i.p.; Male albino mice weighing between 22–30 g) hydrochloride dose-dependently decreases immobility period (in seconds) with respect to vehicle control group. ED50 values of bupropion in reducing the immobility period was found to be 18.5 and 18 mg/kg i.p., in forced swim test and tail suspension test, respectively. Bupropion (10, 20 and 40 mg/kg., i.p.) hydrochloride dose-dependently increases the concentration of free dopamine and its metabolite homovanillic acid in the mouse brain[5].

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

Animal Model: Male Swiss mice weighing 20-25 g[4]
Dosage: 100-160 mg/kg
Administration: IP
Result: Caused clonic convulsions, with the CD50 and CD97 being 119.7 (104.1-137.6) and 156.7 mg/kg, respectively.
When given at a full convulsant dose of 160 mg/kg, the median latency was 6.00 min (3.50-8.15). Tonic convulsions were observed occasionally (1 per 8 mice) only in the groups receiving 140 or 160 mg/kg.
分子量

276.20

Formula

C13H19Cl2NO

CAS 号
性状

固体

颜色

White to off-white

中文名称

盐酸安非他酮;盐酸安非布他酮;盐酸丁氨苯丙酮

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 : 33.33 mg/mL (120.67 mM; 超声助溶 (<80°C); 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

H2O 中的溶解度 : 5.56 mg/mL (20.13 mM; 超声助溶 (<80°C))

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.6206 mL 18.1028 mL 36.2056 mL
5 mM 0.7241 mL 3.6206 mL 7.2411 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。

* 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

  • 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 (9.05 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。

    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% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (9.05 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。

    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 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: 99.94%

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
H2O / DMSO 1 mM 3.6206 mL 18.1028 mL 36.2056 mL 90.5141 mL
5 mM 0.7241 mL 3.6206 mL 7.2411 mL 18.1028 mL
10 mM 0.3621 mL 1.8103 mL 3.6206 mL 9.0514 mL
15 mM 0.2414 mL 1.2069 mL 2.4137 mL 6.0343 mL
20 mM 0.1810 mL 0.9051 mL 1.8103 mL 4.5257 mL
DMSO 25 mM 0.1448 mL 0.7241 mL 1.4482 mL 3.6206 mL
30 mM 0.1207 mL 0.6034 mL 1.2069 mL 3.0171 mL
40 mM 0.0905 mL 0.4526 mL 0.9051 mL 2.2629 mL
50 mM 0.0724 mL 0.3621 mL 0.7241 mL 1.8103 mL
60 mM 0.0603 mL 0.3017 mL 0.6034 mL 1.5086 mL
80 mM 0.0453 mL 0.2263 mL 0.4526 mL 1.1314 mL
100 mM 0.0362 mL 0.1810 mL 0.3621 mL 0.9051 mL

* 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

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.

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