AR-M 1000390

Cat. No.: HY-101039: FAQs
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AR-M 1000390 is an exceptionally selective, potent δ opioid receptor agonist with an EC₅₀ of 7.2±0.9 nM for δ agonist potency.

For research use only. We do not sell to patients.

AR-M 1000390 Chemical Structure

CAS No. : 209808-01-5

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Other In-stock Forms of AR-M 1000390:

AR-M 1000390 hydrochloride

Other Forms of AR-M 1000390:

AR-M 1000390 hydrochloride In-stock

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μ Opioid Receptor/MOR κ Opioid Receptor/KOR δ Opioid Receptor/DOR NOP Receptor/ORL1

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Description	AR-M 1000390 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]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. AR-M 1000390 Related Antibodies
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]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight	348.48
Formula	C₂₃H₂₈N₂O
CAS No.	209808-01-5
SMILES	O=C(N(CC)CC)C1=CC=C(/C(C2=CC=CC=C2)=C3CCNCC/3)C=C1
Shipping	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation	Data Sheet (274 KB) Handling Instructions (2659 KB)
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. [Content Brief] [2]. Otieno MA, et al. Mechanistic investigation of N,N-diethyl-4-(phenyl-piperidin-4-ylidenemethyl)-benzamide-inducedinsulin depletion in the rat and RINm5F cells. Toxicol Sci. 2008 Sep;105(1):221-9. [Content Brief]

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	[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. [Content Brief] [2]. Otieno MA, et al. Mechanistic investigation of N,N-diethyl-4-(phenyl-piperidin-4-ylidenemethyl)-benzamide-inducedinsulin depletion in the rat and RINm5F cells. Toxicol Sci. 2008 Sep;105(1):221-9. [Content Brief]

AR-M 1000390 Related Classifications

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Do most proteins show cross-species activity?
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Keywords:

AR-M 1000390209808-01-5Opioid ReceptorInhibitorinhibitorinhibit

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AR-M 1000390

Other Forms of AR-M 1000390:

AR-M 1000390 Related Antibodies

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Biological Activity

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