AR-M 1000390 hydrochloride
mRNA synthesis
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.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
AR-M 1000390 hydrochloride是δ阿片受体的有效选择性激动剂,IC50值为0.87 nM [1]。
阿片受体是G蛋白偶联受体,阿片是其配体。δ阿片受体是阿片受体,脑啡肽作为其内源性配体,活化δ阿片受体可引起镇痛效果。
AR-M 1000390 hydrochloride是δ阿片受体的有效选择性激动剂,对δ阿片受体、μ阿片受体和κ阿片受体的IC50值分别为0.87 nM、3.8和7.47 μM [1]。在SK-N-BE神经母细胞瘤细胞系中,AR-M 1000390抑制forskolin刺激的cAMP累积,Ki和EC50值分别为106和111 nM。AR-M1000390持续激活阿片受体,产生强烈的脱敏[2]。
在DOR-eGFP小鼠中,第1天,10 mg/kg 的ARM390显著降低CFA诱导的热痛觉过敏,并在第5天诱导完整耐受性,在ARM390耐受小鼠中,背根神经节中的δ阿片受体与钙离子通道解耦联[3]。
参考文献:
[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.
Physical Appearance | White solid |
Storage | Store at -20°C |
M.Wt | 384.94 |
Cas No. | 209808-47-9 |
Formula | C23H28N2O·HCl |
Solubility | <38.49mg/ml in DMSO; <38.49mg/ml in H2O |
Chemical Name | N,N-diethyl-4-(phenyl(piperidin-4-ylidene)methyl)benzamide hydrochloride |
SDF | Download SDF |
Canonical SMILES | O=C(C1=CC=C(C=C1)/C(C2=CC=CC=C2)=C3CCNCC/3)N(CC)CC.Cl |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |