貨號	規格	價格	上海	北京	武漢	南京
S29691-5mg	99.7%	￥650.00 S29691-5mg ￥650.00 現貨	7 7	-	-	-
S29691-10mg	99.7%	￥1000.00 S29691-10mg ￥1000.00 現貨	5 5	-	-	-
S29691-25mg	99.7%	￥2000.00 S29691-25mg ￥2000.00 現貨	6 6	-	-	-
S29691-100mg	99.7%	￥5600.00 S29691-100mg ￥5600.00 現貨	3 3	-	-	-

產品介紹

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.

產品描述：

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.

靶點：

EC50: 7.2±0.9 nM (δ opioid receptor);OpioidReceptor

體外研究：

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). 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).

體內研究：

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.

參考文獻：

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.
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.

溶解性：

Soluble in DMSO、H2O

保存條件：

2-8℃

配置溶液濃度參考：

	1mg	5mg	10mg
1 mM	2.598 ml	12.989 ml	25.978 ml
5 mM	0.52 ml	2.598 ml	5.196 ml
10 mM	0.26 ml	1.299 ml	2.598 ml
50 mM	0.052 ml	0.26 ml	0.52 ml

注意：

部分產品我司僅能提供部分信息，我司不保證所提供信息的權威性，僅供客戶參考交流研究之用。

參考文獻

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ARM390 HCl

N,N-Diethyl-4-(phenyl-4-piperidinylidenemethyl)benzamide Hydrochloride