SB-612111 是一种新型高效的人阿片受体孤儿受体 (ORL-1) 拮抗剂，对 hORL-1 具有较高的亲和力 (Ki=0.33 nM)。SB-612111 对 μ-，κ- 和 δ-receptor 的 Ki 值分别为 57.6 nM，160.5 nM 和 2109 nM。SB-612111 能有效拮抗 Nociceptin 在急性疼痛模型中的造成的痛觉作用。
| Cas No. | 371980-98-2 |
| 别名 | (5S,7S)-7-[[4-(2,6-二氯苯基)-1-哌啶基]甲基]-6,7,8,9-四氢-1-甲基-5H-苯并环庚烯-5-醇 |
| Canonical SMILES | O[C@H]1C[C@@H](CN2CCC(C3=C(Cl)C=CC=C3Cl)CC2)CCC4=C(C)C=CC=C41 |
| 分子式 | C24H29Cl2NO |
| 分子量 | 418.4 |
| 溶解度 | Soluble in DMSO |
| 储存条件 | Store at -20°C |
| 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 | SB-612111 is a novel and potent human opiate receptor-like orphan receptor (ORL-1) antagonist with a high affinity for hORL-1 (Ki=0.33 nM). SB-612111 exhibits selectivity for μ-, κ- and δ-receptors with Ki values of 57.6 nM, 160.5 nM and 2109 nM, respecticely. SB-612111 effectively antagonizes the pronociceptive action of Nociceptin in an acute pain model[1]. [1]. Paola F Zaratin, et al. Modification of Nociception and Morphine Tolerance by the Selective Opiate Receptor-Like Orphan Receptor Antagonist (-)-cis-1-methyl-7-[[4-(2,6-dichlorophenyl)piperidin-1-yl]methyl]-6,7,8,9-tetrahydro-5H-benzocyclohepten-5-ol (SB-612111).J Pharmacol Exp Ther. 2004 Feb;308(2):454-61. |
