| 货号 | 规格 | 价格 | 上海 | 北京 | 武汉 | 南京 | 购买数量 |
|---|---|---|---|---|---|---|---|
S29691-5mg |
99.7% | ￥650.00 | 7 | - | - | - |
|
S29691-10mg |
99.7% | ￥1000.00 | 5 | - | - | - |
|
S29691-25mg |
99.7% | ￥2000.00 | 6 | - | - | - |
|
S29691-100mg |
99.7% | ￥5600.00 | 3 | - | - | - |
|
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.
| 产品描述： | 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. | ||||||||||||||||||||
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| 靶点： | EC50: 7.2±0.9 nM (δ opioid receptor);OpioidReceptor | ||||||||||||||||||||
| 体外研究： | 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). | ||||||||||||||||||||
| 体内研究： | 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. | ||||||||||||||||||||
| 参考文献： | 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. |
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| 溶解性： | Soluble in DMSO、H2O | ||||||||||||||||||||
| 保存条件： | 2-8℃ | ||||||||||||||||||||
| 配置溶液浓度参考： |
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| 注意： | 部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
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