A μ-opioid receptor antagonist
Related Products
Active Metabolite(s)
34298ADL 08-0011 (hydrochloride)
Labeled Version(s)
33812Alvimopan-d5
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Alvimopan

Item No. 23902

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[(2S)-2-[[(3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethyl-1-piperidinyl]methyl]-1-oxo-3-phenylpropyl]-glycine
CAS Number
156053-89-3
Synonyms
  • ADL 8-2698
  • LY246736
Molecular Formula
C25H32N2O4
Formula Weight
424.5
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 10 mg/mlDMSO: 20 mg/mlDMSO:PBS (pH 7.2) (1:3): 0.25 mg/ml
SMILES
OC1=CC=CC([C@]2(C)CCN(C[C@@H](C(NCC(O)=O)=O)CC3=CC=CC=C3)C[C@@H]2C)=C1
InChi Code
InChI=1S/C25H32N2O4/c1-18-16-27(12-11-25(18,2)21-9-6-10-22(28)14-21)17-20(24(31)26-15-23(29)30)13-19-7-4-3-5-8-19/h3-10,14,18,20,28H,11-13,15-17H2,1-2H3,(H,26,31)(H,29,30)/t18-,20-,25+/m0/s1
InChi Key
UPNUIXSCZBYVBB-JVFUWBCBSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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Certificates of Analysis & Batch Specific Data

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    5 mg

    $108

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    10 mg

    $184

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    25 mg

    $378

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    100 mg

    $1,294

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    Product Description

    Alvimopan is a μ-opioid receptor antagonist (Ki = 0.47 nM).1 It is selective over the κ- and δ-opioid receptors (Kis= 100 nM and 12 nM, respectively). Alvimopan inhibits μ-opioid receptor-mediated GTP binding to CHO cell membranes with an IC50 value of 1.7 nM. It inhibits morphine-induced slowing of colorectal transit in mice with an ED50 value of 0.41 mg/kg.2 Alvimopan (0.3 and 1 mg/kg, p.o.) reduces inhibition of gastrointestinal (GI) transit induced by morphine, but not apraclonidine (Item No. 23904), in rats. Formulations containing alvimopan have been used in the treatment of opioid-induced bowel dysfunction.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Le Bourdonnec, B., Barker, W.M., Belanger, S., et al. Novel trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidines as μ opioid receptor antagonists with improved opioid receptor selectivity profiles. Bioorg. Med. Chem. Lett. 18(6), 2006-2012 (2008).

    2. Greenwood-Van Meerveld, B., Gardner, C.J., Little, P.J., et al. Preclinical studies of opioids and opioid antagonists on gastrointestinal function. Neurogastroenterol. Motil. 16(Suppl. 2), 46-53 (2004).

    Product Citations

    Khan, S., Tyson, A.S., Ranjbar, M., et al. Structural snapshots capture nucleotide release at the μ-opioid receptor. Nature (2025).