AR-M 1000390 hydrochloride
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
AR-M 1000390 hydrochloride is a potent and selective agonist of δ-opioid receptor with IC50 value of 0.87 nM .
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 . 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 .
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 .
. 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.
. 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.
. 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.
|Physical Appearance||White solid|
|Storage||Store at -20°C|
|Solubility||<38.49mg/ml in DMSO; <38.49mg/ml in H2O|
|Chemical Name||N,N-diethyl-4-(phenyl(piperidin-4-ylidene)methyl)benzamide hydrochloride|
|Shipping Condition||Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request|
|General tips||For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.|