Alvimopan (monohydrate)
CAS No. : 1383577-62-5
(Synonyms: ADL 8-2698 monohydrate; LY 246736 monohydrate)
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| Cat. No. : | HY-76657 |
| M.Wt: | 442.55 |
| Formula: | C25H34N2O5 |
| Purity: | >98 % |
| Solubility: | 10 mM in DMSO |
Alvimopan monohydrate (ADL 8-2698 monohydrate) is a potent, selective, orally active and reversible μ-opioid receptor antagonist, with an IC50 of 1.7 nM. Alvimopan monohydrate has selectivity for μ-opioid receptor (Ki=0.47 nM) over κ- and δ-opioid receptors (Kis=100, 12 nM, respectively). Alvimopan monohydrate can be used for the research of postoperative ileus[1][2][3].
IC50 & Target: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 in rats[3].
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].
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