货号:A114778 同义名: 阿尔维莫潘 / LY 246736;ADL 8-2698
Alvimopan is a peripherally selective opioid mu receptor antagonist.
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Type | HazMat fee for 500 gram (Estimated) |
Excepted Quantity | USD 0.00 |
Limited Quantity | USD 15-60 |
Inaccessible (Haz class 6.1), Domestic | USD 80+ |
Inaccessible (Haz class 6.1), International | USD 150+ |
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Accessible (Haz class 3, 4, 5 or 8), International | USD 200+ |
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产品名称 | Opioid receptor ↓ ↑ | ORL1 ↓ ↑ | μ-opioid receptor ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Racecadotril | ✔ | 98% | |||||||||||||||||
JTC-801 |
++
Opioid receptor-like1 (ORL1), IC50: 94 nM |
98% | |||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
描述 | Alvimopan is a potent, selective, orally active and reversible μ-opioid receptor antagonist, with an IC50 of 1.7 nM[3]. Alvimopan has a greater affinity for the mu-receptor than the kappa- or sigma-opioid receptors (Ki = 0.77 nM). It has limited systemic bioavailability and higher affinity for the mu-opioid receptor than naloxone (Ki = 3.7 nM)[4]. 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 behavioral responses (VMR) induced by noxious colorectal distension (CRD) in conscious rats[5]. Alvimopan showed significant advantages over placebo in restoring gastro-intestinal function, and reduced time to discharge following major abdominal surgery, with acceptable side effects[6]. Alvimopan significantly reduced the incidence of ileus and NGT (nasogastric tube) placement following RC(radical cystectomy). NGT placement was associated with an increased need for reoperation for bowel complications in the setting of alvimopan[7]. |
NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
NCT02109640 | Postoperative Pain ... 展开 >> Postoperative Nausea and Vomiting 收起 << | Phase 3 | Completed | - | United Kingdom ... 展开 >> Western General Hospital Edinburgh, United Kingdom, EH4 2XU 收起 << |
NCT02109640 | - | Completed | - | - | |
NCT00388479 | Ileus | Phase 3 | Completed | - | United States, Pennsylvania ... 展开 >> Various Exton, Pennsylvania, United States, 19341 收起 << |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.36mL 0.47mL 0.24mL |
11.78mL 2.36mL 1.18mL |
23.56mL 4.71mL 2.36mL |
CAS号 | 156053-89-3 |
分子式 | C25H32N2O4 |
分子量 | 424.533 |
别名 | 阿尔维莫潘 ;LY 246736;ADL 8-2698;Alvimopan. trade name Entereg.;HSDB 7704 |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Sealed in dry,2-8°C |
溶解度 | |
动物实验配方 |