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Alvimopan Opioid Receptor antagonist

Name: Alvimopan
Brand: Selleck Chemicals
SKU: S5935
Availability: InStock
Rating: 5 (1 reviews)

Cat.No.S5935

Alvimopan (LY 246736, ADL 8-2698) is a potent, relatively nonselective opioid antagonist with Ki 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.

Chemical Structure

Molecular Weight: 424.53

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Quality Control

Batch: Purity: 99.64%

99.64

Related Targets	Adrenergic Receptor AChR 5-HT Receptor COX Calcium Channel Histamine Receptor Dopamine Receptor GABA Receptor TRP Channel Cholinesterase (ChE)
Other Opioid Receptor Inhibitors	JTC-801 (+)-Matrine Asimadoline hydrochloride BMS-986122 Racecadotril Aticaprant Trimebutine maleate Naloxegol Oxalate Docusate Sodium methylnaltrexone bromide

Solubility

In vitro
Batch:

DMSO : 85 mg/mL (200.22 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	4.250mg/ml (10.01mM)	Taking the 1 mL working solution as an example, add 50 μL of 85 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.600mg/ml (1.41mM)	Taking the 1 mL working solution as an example, add 50 μL of 12 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	424.53	Formula	C₂₅H₃₂N₂O₄	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	156053-89-3	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	LY 246736, ADL 8-2698			Smiles	CC1CN(CCC1(C)C2=CC(=CC=C2)O)CC(CC3=CC=CC=C3)C(=O)NCC(=O)O

Mechanism of Action

Targets/IC₅₀/Ki	μ-opioid receptor (Cell-free assay) 0.77 nM(Ki) δ-opioid receptor (Cell-free assay) 4.4 nM δ-opioid receptor (Cell-free assay) 4.4 nM(Ki) κ-opioid receptor (Cell-free assay) 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, this compound 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 this chemical are lower in the guinea pig ileum (pA2 values of 8.7 and 7.8, respectively). This compound (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.
In vivo	In animals, alvimopan antagonizes centrally mediated, morphine-induced analgesia only at relatively high doses, with very high plasma concentrations needed to cross the blood-brain barrier. After intravenous administration, this compound is approximately 200-times more potent at blocking peripheral verses central μ-receptors. After oral administration, it is also highly active. In dogs, intravenous administration of this chemical provided dose-dependent increases in peak plasma concentrations and plasma area under the concentration-time curve. However, as a result of poor systemic absorption, oral doses up to 100 mg/kg produced low plasma concentrations (mean Cmax =92.9 ng/ml), which resulted in an oral bioavailability of approximately 0.03%. The half-life of this agent is estimated to be approximately 10 min after intravenous administration in dogs and rabbits.
References	[1] https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2730789/ [2] http://journals.sagepub.com/doi/full/10.4137/CMT.S2384

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT03068975	Terminated	Post Operative Ileus	University of Puerto Rico\|Merck Sharp & Dohme LLC	September 1 2017	Phase 4
NCT00259922	Completed	Bowel Dysfunction\|Constipation	Cubist Pharmaceuticals LLC a subsidiary of Merck & Co. Inc. (Rahway New Jersey USA)\|GlaxoSmithKline	August 2005	Phase 3
NCT00256932	Completed	Bowel Dysfunction\|Constipation	Cubist Pharmaceuticals LLC a subsidiary of Merck & Co. Inc. (Rahway New Jersey USA)\|GlaxoSmithKline	August 2005	Phase 3
NCT00241722	Completed	Bowel Dysfunction\|Constipation	Cubist Pharmaceuticals LLC a subsidiary of Merck & Co. Inc. (Rahway New Jersey USA)\|GlaxoSmithKline	August 1 2005	Phase 3

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