1. GPCR/G Protein Neuronal Signaling
  2. Opioid Receptor
  3. Norbinaltorphimine dihydrochloride

Norbinaltorphimine dihydrochloride  (Synonyms: nor-Binaltorphimine dihydrochloride; nor-BNI dihydrochloride)

目录号: HY-100903 纯度: 98.17%
COA 产品使用指南

Norbinaltorphimine dihydrochloride是一种有效的和选择性的κ阿片受体 (κ opioid receptor) 拮抗剂。

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Norbinaltorphimine dihydrochloride Chemical Structure

Norbinaltorphimine dihydrochloride Chemical Structure

CAS No. : 113158-34-2

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥1560
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5 mg ¥950
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10 mg ¥1500
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50 mg ¥5200
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Customer Review

Other Forms of Norbinaltorphimine dihydrochloride:

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

Norbinaltorphimine dihydrochloride is a potent and selective κ opioid receptor antagonist.

IC50 & Target

κ Opioid Receptor/KOR

 

体外研究
(In Vitro)

Norbinaltorphimine reversibly antagonize the effects of κ agonists with pA2 values of 10.2-10.4. Norbinaltorphimine is much less potent as an antagonist at μ and δ receptors, pA2 values are 7.4-7.6 and 7.6-7.8, respectively[1].

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

体内研究
(In Vivo)

Norbinaltorphimine has weak and inconsistent effects on THC-induced taste avoidance in adolescent rats in that Norbinaltorphimine both attenuates and strengthens taste avoidance dependent on dose and trial. Norbinaltorphimine has limited impact on the final one-bottle avoidance and no effects on the two-bottle preference test. Interestingly, Norbinaltorphimine has no effect on THC-induced taste avoidance in adult rats as well[2]. Norbinaltorphimine pretreatment significantly attenuates stress-induced reinstatement of nicotine-CPP, but has no effect on nicotine-primed reinstatement[3].

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

分子量

734.71

Formula

C40H45Cl2N3O6

CAS 号
性状

固体

颜色

Light yellow to gray

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 (136.11 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)

H2O 中的溶解度 : 33.33 mg/mL (45.36 mM; 超声助溶)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.3611 mL 6.8054 mL 13.6108 mL
5 mM 0.2722 mL 1.3611 mL 2.7222 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 (3.40 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 (3.40 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
计算结果
工作液所需浓度 : mg/mL
该产品水溶性佳,请具体参考实测 水 / PBS / Saline 中的溶解度数据。
您所需的储备液浓度超过该产品的实测溶解度,如有需要,请与 MCE 中国技术支持联系。
纯度 & 产品资料

纯度: 98.17%

参考文献
Animal Administration
[2][3]

Rats[2]

Norbinaltorphimine is dissolved in sterile H2O at a concentration of 15 mg/mL and administered subcutaneously (SC) at a dose of 15 mg/kg. Male Sprague Dawley rats are ranked according to average water consumption on all habituation cycles and assigned to one of two groups [Norbinaltorphimine (n=42) and Vehicle (n=42)], such that mean water intake is comparable among groups. On PND 34 (approximately 24 h prior to conditioning, see below), subjects assigned to the Norbinaltorphimine group are injected with Norbinaltorphimine (15 mg/kg) and subjects assigned to the Vehicle group are injected with the Norbinaltorphimine vehicle at an equal volume[2].

Mice[3]

Mice are conditioned with 0.5 mg/kg nicotine, injected subcutaneously (s.c.) for 3 days and tested in the nicotine-conditioned place preference (CPP) model. After 3 days extinction, Norbinaltorphimine (10 mg/kg, s.c.) is administered 16 h prior to a priming dose of nicotine (0.1 mg/kg, s.c.), and mice are tested in the CPP model for nicotine-induced reinstatement of CPP. A separate group of mice is subjected to a 2-day modified forced swim test (FST) paradigm to induce stress after 3 days extinction from CPP. Mice are given vehicle or Norbinaltorphimine (10 mg/kg, s.c.) 16 h prior to each FST session[3].

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

参考文献

Norbinaltorphimine dihydrochloride 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 (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 1.3611 mL 6.8054 mL 13.6108 mL 34.0270 mL
5 mM 0.2722 mL 1.3611 mL 2.7222 mL 6.8054 mL
10 mM 0.1361 mL 0.6805 mL 1.3611 mL 3.4027 mL
15 mM 0.0907 mL 0.4537 mL 0.9074 mL 2.2685 mL
20 mM 0.0681 mL 0.3403 mL 0.6805 mL 1.7014 mL
25 mM 0.0544 mL 0.2722 mL 0.5444 mL 1.3611 mL
30 mM 0.0454 mL 0.2268 mL 0.4537 mL 1.1342 mL
40 mM 0.0340 mL 0.1701 mL 0.3403 mL 0.8507 mL
DMSO 50 mM 0.0272 mL 0.1361 mL 0.2722 mL 0.6805 mL
60 mM 0.0227 mL 0.1134 mL 0.2268 mL 0.5671 mL
80 mM 0.0170 mL 0.0851 mL 0.1701 mL 0.4253 mL
100 mM 0.0136 mL 0.0681 mL 0.1361 mL 0.3403 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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Norbinaltorphimine dihydrochloride
目录号:
HY-100903
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