Alvimopan dihydrate/ADL 8-2698 dihydrate；爱维莫潘二水合物
货号：
IA2140
品牌：
Jinpan
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产品简介
| MDL | MFCD26142939 |
| 别名 | ADL8-2698dihydrate;LY246736dihydrate |
| 英文名称 | Alvimopan dihydrate/ADL 8-2698 dihydrate |
| CAS | 170098-38-1 |
| 分子式 | C25H36N2O6 |
| 分子量 | 460.56 |
| 纯度 | ≥98% |
| 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 | OC1=CC=CC([C@@]2(C)[C@@H](C)CN(C[C@H](CC3=CC=CC=C3)C(NCC(O)=O)=O)CC2)=C1.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 50mg |
是一种有效的、相对非选择性的opioid拮抗剂