[CAS NO. 156053-89-3] Alvimopan

Name: Alvimopan
Brand: Arctom Scientific
SKU: SLK-S5935

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PRODUCTS SPECIFICATIONS [156053-89-3]

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Catalog

SLK-S5935

Brand

Selleck

CAS

156053-89-3

DESCRIPTION [156053-89-3]

Overview

MDL	MFCD09838268
Molecular Weight	424.53
Molecular Formula	C25H32N2O4
SMILES	C[C@@]1([C@@H](C)CN(C[C@H](CC2=CC=CC=C2)C(NCC(O)=O)=O)CC1)C3=CC(O)=CC=C3

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	2.3555 mL	11.7777 mL	23.5555 mL
5 mM	0.4711 mL	2.3555 mL	4.7111 mL
10 mM	0.2356 mL	1.1778 mL	2.3555 mL
50 mM	0.0471 mL	0.2356 mL	0.4711 mL

Description

Alvimopan (LY 246736, ADL 8-2698) is a potent, relatively nonselective antagonist with values of 0.77, 4.4, and 40 nM for the μ, δ, and κ opioid receptors, respectively, displaying >100-fold selectivity over other aminergic G-protein-coupled receptors.

Targets

μ-opioid receptor ^[1] (Cell-free assay)	δ-opioid receptor ^[1] (Cell-free assay)	δ-opioid receptor ^[1] (Cell-free assay)	κ-opioid receptor ^[1] (Cell-free assay)
0.77 nM(Ki)	4.4 nM	4.4 nM(Ki)	40 nM(Ki)

In vitro

Alvimopan is highly selective (by ≥227-fold) for the human μ receptor over the κ subtype, but has a more modest (≥6-fold) μ/δ receptor selectivity. In the guinea pig isolated ileum, alvimopan is a potent antagonist of morphine, DAMGO or endomorphin-1-induced, and μ opioid receptor-mediated, inhibition of electrically-evoked contractions (pA2 values of 9.6 or 9.7). The δ and κ antagonist potencies of alvimopan are lower in the guinea pig ileum (pA2 values of 8.7 and 7.8, respectively). Alvimopan (1 or 10 μM) has no significant affinity for a broad range of non-opioid receptors, ion channels and enzymes at which it has been tested.

References

[1] Goldina Ikezuagu Erowele. P T. 2008, 33(10): 574, 580-583.
[2] DT Beattie. Clinical Medicine: Therapeutics. 2009, 1: 199-213.

Synonyms

Glycine, N-[(2S)-2-[[(3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethyl-1-piperidinyl]methyl]-1-oxo-3-phenylpropyl]-

Glycine, N-[2-[[4-(3-hydroxyphenyl)-3,4-dimethyl-1-piperidinyl]methyl]-1-oxo-3-phenylpropyl]-, [3R-[1(S*),3α,4α]]-

N-[(2S)-2-[[(3R,4R)-4-(3-Hydroxyphenyl)-3,4-dimethyl-1-piperidinyl]methyl]-1-oxo-3-phenylpropyl]glycine

LY 246736

ADL 8-2698

Alvimopan

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