1. GPCR/G Protein
    Neuronal Signaling
  2. Opioid Receptor

AR-M 1000390 hydrochloride 

目录号: HY-101039A 纯度: 99.80%
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。

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AR-M 1000390 hydrochloride Chemical Structure

AR-M 1000390 hydrochloride Chemical Structure

CAS No. : 209808-47-9

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Size Price Stock Quantity
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 ¥9950 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Description

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]

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].

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].

Solvent & Solubility
In Vitro: 

DMSO : ≥ 150 mg/mL (389.67 mM)

* "≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 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
10 mM 0.2598 mL 1.2989 mL 2.5978 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (6.49 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.49 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (6.49 mM); Clear solution

References
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.

References
Molecular Weight

384.94

Formula

C₂₃H₂₉ClN₂O

CAS No.

209808-47-9

SMILES

O=C(N(CC)CC)C1=CC=C(/C(C2=CC=CC=C2)=C3CCNCC/3)C=C1.Cl

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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产品名称:
AR-M 1000390 hydrochloride
目录号:
HY-101039A
需求量:

AR-M 1000390 hydrochloride

Cat. No.: HY-101039A