AR-M 1000390 hydrochloride |
| Catalog No.GC12219 |
Delta-opioid receptor agonist,low-internalizing
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 209808-47-9
Sample solution is provided at 25 µL, 10mM.
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AR-M 1000390 hydrochloride is a potent and selective agonist of δ-opioid receptor with IC50 value of 0.87 nM [1].
Opioid receptor is a G protein-coupled receptor with opioids as ligands. δ-opioid receptor is a opioid receptor with enkephalins as its endogenous ligands and activation of δ-opioid receptor causes analgesia.
AR-M 1000390 hydrochloride is a potent and selective δ-opioid receptor agonist with IC50 values of 0.87 nM, 3.8 and 7.47 μM for δ-opioid receptor, μ-opioid receptor and κ-opioid receptor, respectively [1]. In the SK-N-BE neuroblastoma cell line, AR-M 1000390 inhibited forskolin-stimulated cAMP accumulation with Ki and EC50 values of 106 and 111 nM, respectively. Sustained activation of opioid receptors by AR-M1000390 produced a strong desensitization [2].
In DOR-eGFP mice, ARM390 (10 mg/kg) significantly reduced CFA-induced heat hyperalgesia at day 1 and induced complete tolerance at day 5. In ARM390-tolerant mice, δ-opioid receptor uncoupled to Ca2+ channels in dorsal root ganglia [3].
References:
[1]. Wei ZY, Brown W, Takasaki B, et al. N,N-Diethyl-4-(phenylpiperidin-4-ylidenemethyl)benzamide: a novel, exceptionally selective, potent delta opioid receptor agonist with oral bioavailability and its analogues. J Med Chem, 2000, 43(21): 3895-3905.
[2]. Marie N, Landemore G, Debout C, et al. Pharmacological characterization of AR-M1000390 at human delta opioid receptors. Life Sci, 2003, 73(13): 1691-1704.
[3]. Pradhan AA, Walwyn W, Nozaki C, et al. Ligand-Directed Trafficking of the -Opioid Receptor In Vivo: Two Paths Toward Analgesic Tolerance. J Neurosci, 2010, 30(49): 16459-16468.
Cell experiment: | 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]. |
Animal experiment: | 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]. |
References: [1]. Wei ZY, et al. N,N-Diethyl-4-(phenylpiperidin-4-ylidenemethyl)benzamide: a novel, exceptionally selective, potent delta opioid receptor agonist with oral bioavailability and its analogues. J Med Chem. 2000 Oct 19;43(21):3895-905. | |
| Cas No. | 209808-47-9 | SDF | |
| Chemical Name | N,N-diethyl-4-(phenyl(piperidin-4-ylidene)methyl)benzamide hydrochloride | ||
| Canonical SMILES | O=C(C1=CC=C(C=C1)/C(C2=CC=CC=C2)=C3CCNCC/3)N(CC)CC.Cl | ||
| Formula | C23H28N2O.HCl | M.Wt | 384.94 |
| Solubility | <38.49mg/ml in DMSO; <38.49mg/ml in Water | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.5978 mL | 12.989 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 |
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 34 reference(s) in Google Scholar.)
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