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Methylnaltrexone bromide

Name: Methylnaltrexone bromide
Brand: TargetMol
SKU: T21422
Price: 47 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T21422Cas No. 73232-52-7

Alias Relistor, MOA-728, MOA728, MOA 728, Methylnaltrexone

Methylnaltrexone bromide (MOA-728) is one of the newer agents of peripherally-acting μ-opioid antagonists. Methylnaltrexone bromide acts to reverse some of the side effects of opioid drugs such as constipation without affecting analgesia or precipitating withdrawals.

Methylnaltrexone bromide

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Purity: 99.02%

Catalog No. T21422Alias Relistor, MOA-728, MOA728, MOA 728, MethylnaltrexoneCas No. 73232-52-7

Pack Size	Price	USA Warehouse	Global Warehouse
2 mg	$47	In Stock	In Stock
5 mg	$77	In Stock	In Stock
10 mg	$118	In Stock	In Stock
25 mg	$200	In Stock	In Stock
50 mg	$286	In Stock	In Stock
100 mg	$497	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$91	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Purity:99.02%

Color:White

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COA HNMR LCMS

Product Introduction

Methylnaltrexone bromide AI Summary

Methylnaltrexone bromide exhibits potent bioactivities related to opioid receptors. It is a high-affinity mu-opioid receptor agonist (Ki = 5.48 nM for [3H]-DAMGO displacement) and also demonstrates antagonist properties at this receptor (Ke = 56.0 nM in the [35S]-GTPgammaS binding assay). Additionally, it has lower affinity as a delta-opioid receptor agonist (Ki = 3460.0 nM for [3H]-DADLE displacement) and antagonistic activity (Ke = 1080.0 nM in the [35S]-GTPgammaS binding assay). In vivo studies reveal that Methylnaltrexone bromide acts as an antagonist at both mu-opioid and delta-opioid receptors, effectively inhibiting morphine-induced emesis (ED50 = 0.69 mg/kg) and constipation (ED50 = 4.5 mg/kg) in animal models. It shows no induction of drug-induced liver injury in human subjects, indicating no liver toxicity. The compound also demonstrates oral bioavailability in both humans and rats, with variable absorption and half-life. It inhibits morphine-induced delays in gastric emptying and intestinal transit in mice and shows specific binding affinities for kappa, delta, and mu opioid receptors in different cell membranes..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description	Methylnaltrexone bromide (MOA-728) is one of the newer agents of peripherally-acting μ-opioid antagonists. Methylnaltrexone bromide acts to reverse some of the side effects of opioid drugs such as constipation without affecting analgesia or precipitating withdrawals.
Synonyms	Relistor, MOA-728, MOA728, MOA 728, Methylnaltrexone

Chemical Properties

Molecular Weight	436.35
Formula	C₂₁H₂₆BrNO₄
Cas No.	73232-52-7
Smiles	O=C1[C@@](OC2=C(O)C=CC3=C24)([H])[C@@]54CC[N+](C)(CC6CC6)[C@@](C3)([H])[C@]5(O)CC1.[Br-]
Relative Density.	no data available

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

H2O: Insoluble

DMSO: 60 mg/mL (137.5 mM), Sonication is recommended.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.2917 mL	11.4587 mL	22.9174 mL	114.5869 mL
5 mM	0.4583 mL	2.2917 mL	4.5835 mL	22.9174 mL
10 mM	0.2292 mL	1.1459 mL	2.2917 mL	11.4587 mL
20 mM	0.1146 mL	0.5729 mL	1.1459 mL	5.7293 mL
50 mM	0.0458 mL	0.2292 mL	0.4583 mL	2.2917 mL
100 mM	0.0229 mL	0.1146 mL	0.2292 mL	1.1459 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc