AR-M 1000390 hydrochloride,99.05%
产品编号:Bellancom-101039A| CAS NO:209808-47-9| 分子式:C23H29ClN2O| 分子量:384.94
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AR-M 1000390 hydrochloride
产品介绍 | AR-M 1000390 hydrochloride 是一种有效的选择性 δ 阿片受体激动剂,EC50 为 7.2±0.9 nM。 | ||||||||||||||||
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生物活性 | 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. | ||||||||||||||||
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). 西域 has not independently confirmed the accuracy of these methods. They are for reference only. | ||||||||||||||||
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. 西域 has not independently confirmed the accuracy of these methods. They are for reference only. | ||||||||||||||||
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. 西域 has not independently confirmed the accuracy of these methods. They are for reference only. | ||||||||||||||||
性状 | Solid | ||||||||||||||||
溶解性数据 |
In Vitro:
DMSO : ≥ 150 mg/mL (389.67 mM) H2O : 50 mg/mL (129.89 mM; Need ultrasonic) * "≥" means soluble, but saturation unknown. 配制储备液
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请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 In Vivo:
请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用;
以下溶剂前显示的百
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运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 |
4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) | ||||||||||||||||
参考文献 |
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