S83881 |
Alvimopan dihydrate (ADL 8-2698 dihydrate) |
源叶(MedMol) | 98% |
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- 产品描述: 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
- 靶点: IC50: 1.7 nM (μ-opioid receptor)
- 体内研究:
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
- 参考文献:
1. Bourdonnec BL, et, al. Novel trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidines as mu opioid receptor antagonists with improved opioid receptor selectivity profiles. Bioorg Med Chem Lett. 2008 Mar 15;18(6):2006-12. 2. Erowele GI, et, al. Alvimopan (Entereg), a Peripherally Acting mu-Opioid Receptor Antagonist For Postoperative Ileus. P T. 2008 Oct;33(10):574-83. 3. Meerveld BG, et, al. Preclinical studies of opioids and opioid antagonists on gastrointestinal function. Neurogastroenterol Motil. 2004 Oct;16 Suppl 2:46-53.
- 溶解性: Soluble in DMSO
- 保存条件: -20℃
- 配置溶液浓度参考:
1mg 5mg 10mg 1 mM 2.171 ml 10.856 ml 21.713 ml 5 mM 0.434 ml 2.171 ml 4.343 ml 10 mM 0.217 ml 1.086 ml 2.171 ml 50 mM 0.043 ml 0.217 ml 0.434 ml
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)