货号:A397796 同义名: LY 246736 dihydrate;ADL 8-2698 dihydrate
Alvimopan is a peripherally acting mu-opioid receptor (PAM-OR, IC50= 1.7 nM) antagonist for accelerating gastrointestinal recovery after surgery.
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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, a peripherally acting mu-opioid receptor antagonist, is a novel agent for the treatment of postoperative ileus[3]. Alvimopan inhibits the loperamide-stimulated [35S]GTPγS binding to membranes containing the cloned human μ-opioid receptor, with an IC50 of 1.7 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 behavioural responses (VMR) induced by noxious colorectal distension (CRD) in conscious rats[5]. Mesenteric afferent fibres are markedly stimulated by mu-opioid receptor agonists, an effect blocked by alvimopan, which may contribute to the gastrointestinal reflex and behavioural responses to opiate treatment or abuse[6]. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.17mL 0.43mL 0.22mL |
10.86mL 2.17mL 1.09mL |
21.71mL 4.34mL 2.17mL |
CAS号 | 170098-38-1 |
分子式 | C25H36N2O6 |
分子量 | 460.563 |
别名 | LY 246736 dihydrate;ADL 8-2698 dihydrate;Alvimopan hydrate;Entereg |
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 |
DMSO: 35 mg/mL(75.99 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
动物实验配方 |