| CAS NO: | 67197-96-0 |
| 包装: | 1mg |
| 市场价: | 1470元 |
κ-opioid receptor agonist, selective
| Cas No. | 67197-96-0 |
| 别名 | (±)-Trans-(1R,2R)-U-50488 hydrochloride |
| 化学名 | 2-(3,4-dichlorophenyl)-N-methyl-N-((1R,2R)-2-(pyrrolidin-1-yl)cyclohexyl)acetamide hydrochloride |
| Canonical SMILES | CN(C(CC1=CC(Cl)=C(Cl)C=C1)=O)[C@]2([H])CCCC[C@@]2([H])N3CCCC3.Cl |
| 分子式 | C19H26Cl2N2O.HCl |
| 分子量 | 405.79 |
| 溶解度 | 20mg/mL in DMSO, 20mg/mL in DMF, 20mg/mL in Ethanol |
| 储存条件 | Desiccate at -20℃ |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
| 产品描述 | (±)-U-50488 hydrochloride is a selective agonist for κ-opioid receptor [1]. The κ-opioid receptor (KOR) is a type of opioid receptor for opioid peptide dynorphin and controls addiction. Also, KOR plays an important role in stress, anxiety, anhedonia, depression and increased drug-seeking behavior. (±)-U-50488 hydrochloride is a selective KOR agonist [1]. In isolated rat DRG neurons, U-50488 (0.3-40 μM) inhibited voltage-independent Ca2+ channel currents. In HeLa cells that didn’t express KOR, U-50488 (20 μM) blocked Ca2+ channels [2]. In rhesus monkeys, U-50488 exhibited potent antinociceptive activity and produced diuresis [1]. U-50488 enhanced contraction of the rabbit vas deferens induced by electrically with IC50 value of 26.5 nM. In mice, U-50488 impaired motor function with ED50 value of 15.3 mg/kg and reduced spontaneous activity [3]. In adult rats, U-50488 increased the threshold required to maintain self-stimulation responding, a depressive-like effect. While, males were significantly more sensitive than females to the threshold-increasing effects [4]. References: |
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