BMS 986122 是一种选择性、强效的 mu-阿片受体 (μ-OR) 正变构调节剂。
| Cas No. | 313669-88-4 |
| Canonical SMILES | COC1=CC=C(C2N(S(C3=CC=C(Cl)C=C3)(=O)=O)CCS2)C=C1Br |
| 分子式 | C16H15BrClNO3S2 |
| 分子量 | 448.8 |
| 溶解度 | DMF: 10 mg/ml,DMSO: 10 mg/ml,DMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml,Ethanol: 2 mg/ml |
| 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 | BMS 986122 is a positive allosteric modulator of μ-opioid receptors that increases β-arrestin recruitment stimulated by endomorphin 1 in U2OS-OPRM1 human osteosarcoma cells expressing μ-opioid receptors (EC50 = 3 μM). It potentiates endomorphin 1-induced inhibition of forskolin-stimulated adenylyl cyclase activity in CHO cells expressing human recombinant μ-opioid receptors (EC50 = 8.9 μM). BMS 986122 also enhances [35S]GTPγ binding stimulated by the μ-opioid agonist DAMGO by 7- and 4.5-fold in C6μ glioma cell membranes that express μ-opioid receptors and mouse brain membranes, respectively. |
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