爱维莫潘
货号：
IA3250
品牌：
Jinpan
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产品简介
| 有效期 | 2年 |
| 描述 | 是一种阿片样受体（PAM-OR）拮抗剂。 |
| MDL | MFCD09838268 |
| 别名 | 2-([(2S)-2-([(3R,4R)-4-(3-羟基苯基)-3,4-二甲基哌啶-1-基]甲基)-3-苯基丙酰]氨基)乙酸 |
| 英文名称 | Alvimopan |
| CAS | 156053-89-3 |
| 分子式 | C25H32N2O4 |
| 分子量 | 424.53 |
| 储存条件 | -20℃ |
| 纯度 | ≥98% |
| 外观（性状） | White to off-white Solid |
| 单位 | 瓶 |
| 生物活性 | Alvimopan dihydrate (ADL 8-2698 dihydrate) is a potent, selective, orally active and reversible μ-opioid receptor antagonist, with an IC50 of 1.7 nM. Alvimopan dihydrate has selectivity for μ-opioid receptor (Ki=0.47 nM) over κ- and δ-opioid receptors (Kis=100, 12 nM, respectively). Alvimopan dihydrate can be used for the research of postoperative ileus[1-[3]. |
| IC50 | 1.7 nM (μ-opioid receptor)[1] |
| In Vitro | Alvimopan inhibits the loperamide-stimulated [35S]GTPγS binding to membranes containing the cloned human μ-opioid receptor, with an IC50 of 1.7 nM[1]. |
| In Vivo | Alvimopan (0.1-1.0 mg/kg; p.o.) partially antagonizes the slowing of small intestinal transit of 113Sn-labelled microspheres produced by morphine in rats.Alvimopan (3 mg/kg; p.o.) has no effect on the visceromotor behavioural responses (VMR) induced by noxious colorectal distension (CRD) in conscious rats[3]. |
| SMILES | O=C(CNC([C@@H](CC1=CC=CC=C1)CN2C[C@@H]([C@](C3=CC=CC(O)=C3)(CC2)C)C)=O)O |
| 靶点 | Opioid Receptor |
| 数据来源文献 | [1] Goldina Ikezuagu Erowele. P T. 2008, 33(10): 574, 580-583. [2] DT Beattie. Clinical Medicine: Therapeutics. 2009, 1: 199-213. |
| 规格 | 5mg 10mg |