1. GPCR/G Protein Neuronal Signaling
  2. Opioid Receptor
  3. AR-M 1000390 hydrochloride

AR-M 1000390 hydrochloride 

目录号: HY-101039A 纯度: 99.05%
COA 产品使用指南

AR-M 1000390 hydrochloride 是一种有效的选择性 δ 阿片受体激动剂,EC50 为 7.2±0.9 nM。

MCE 的所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

AR-M 1000390 hydrochloride Chemical Structure

AR-M 1000390 hydrochloride Chemical Structure

CAS No. : 209808-47-9

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2.  同一机构(单位)同一产品试用装仅限申领一次,同一机构(单位)一年内

     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥1089
In-stock
5 mg ¥990
In-stock
10 mg ¥1700
In-stock
50 mg ¥5900
In-stock
100 mg 现货 询价
200 mg   询价  
500 mg   询价  

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Customer Review

Other Forms of AR-M 1000390 hydrochloride:

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

AR-M 1000390 hydrochloride is an exceptionally selective, potent δ opioid receptor agonist with an EC50 of 7.2±0.9 nM for δ agonist potency.

IC50 & Target

EC50: 7.2±0.9 nM (δ opioid receptor)[1]

体外研究
(In Vitro)

AR-M 1000390 (Compound 6a) exhibits the binding affinities (IC50) of 0.87±0.23 nM for the δ opioid receptor and extremely high selectivity over the µ receptor (IC50=3800±172 nM) and the κ receptor (IC50=7470±606 nM)[1]. RINm5F cells are treated with AR-M 1000390 (AR-M100390) and Cyclizine for 16-24 h before measurement of intracellular and secreted insulin levels. AR-M 1000390 mediates a dose-dependent decrease in insulin content with a maximal inhibition of ~90% at the highest concentration tested (10 μM)[2].

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

体内研究
(In Vivo)

Rats are treated with 5, 100, and 600 μmol/kg of AR-M 1000390 (AR-M100390) for 3 and/or 7 days; another group of rats treated with 600 μmol/kg of compound are allowed to recover for 14 days. AR-M 1000390 (600 μmol/kg) causes vacuolation in the β-cell of the rat pancreas that is associated with depletion of insulin and hyperglycemia after 7 days of dosing. Treatment of rats with 600 μmol/kg of AR-M 1000390 results in vacuolation of the β-cell of the rat pancreas that is similar to that reported for cyclizine and cyproheptadine[2].

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

分子量

384.94

Formula

C23H29ClN2O

CAS 号
性状

固体

颜色

White to off-white

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 : ≥ 150 mg/mL (389.67 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)

H2O 中的溶解度 : 50 mg/mL (129.89 mM; 超声助溶)

* "≥" 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 2.5978 mL 12.9890 mL 25.9781 mL
5 mM 0.5196 mL 2.5978 mL 5.1956 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 (6.49 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 (6.49 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: 99.05%

参考文献
Cell Assay
[2]

RINm5F cells are seeded in 24-well plates and treated with vehicle (DMSO), 10 μM AR-M 1000390 (AR-M100390), and 10 μM Cyclizine in serum-free medium; cells are rinsed with phosphate-buffered saline and stored at -80°C until analysis. RNA is isolated with the RNeasy purification system with DNAse treatment[2].

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

Animal Administration
[2]

Rats[2]
Han Wistar rats (six per treatment group) are treated with vehicle (saline) or 5, 100, and 600 μmol/kg/day of AR-M 1000390 (AR-M100390) for 7 days. A separate group of rats are treated with 600 μmol/kg/day for 7 days followed by a 14-day recovery period. Another group is treated with 600 μmol/kg/day for 3 days. Blood sampling for glucose, lipids, and insulin measurements are taken on days 2, 4, 8, and 22. Blood sampling for AR-M 1000390 concentration measurements are collected on days 4 and 8. The animals are euthanized with CO2 on days 4, 8, and 22 and the pancreas isolated and processed for histopathology, insulin immunohistochemistry, and insulin mRNA analyses[2].

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

参考文献

AR-M 1000390 hydrochloride 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 2.5978 mL 12.9890 mL 25.9781 mL 64.9452 mL
5 mM 0.5196 mL 2.5978 mL 5.1956 mL 12.9890 mL
10 mM 0.2598 mL 1.2989 mL 2.5978 mL 6.4945 mL
15 mM 0.1732 mL 0.8659 mL 1.7319 mL 4.3297 mL
20 mM 0.1299 mL 0.6495 mL 1.2989 mL 3.2473 mL
25 mM 0.1039 mL 0.5196 mL 1.0391 mL 2.5978 mL
30 mM 0.0866 mL 0.4330 mL 0.8659 mL 2.1648 mL
40 mM 0.0649 mL 0.3247 mL 0.6495 mL 1.6236 mL
50 mM 0.0520 mL 0.2598 mL 0.5196 mL 1.2989 mL
60 mM 0.0433 mL 0.2165 mL 0.4330 mL 1.0824 mL
80 mM 0.0325 mL 0.1624 mL 0.3247 mL 0.8118 mL
100 mM 0.0260 mL 0.1299 mL 0.2598 mL 0.6495 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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产品名称:
AR-M 1000390 hydrochloride
目录号:
HY-101039A
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