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Alvimopan

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Catalog No. T1242Cas No. 156053-89-3

Alvimopan (LY 246736) is a synthetic trans-3, 4-dimethyl-4-(3-hydroxyphenyl) piperidine with peripherally selective opioid mu receptor antagonist activity. Alvimopan is a selective and competitive antagonist at mu-opioid receptors, found in myenteric and submucosal neurons and the immune cells of the lamina propria in the human gut. Upon administration, this agent binds to mu-opioid receptors in the gut, thereby reversing opioid-related disturbances in gut motility. Alvimopan is approximately three to nine times more potent than naloxone.

Alvimopan

Alvimopan

😃Good
Purity: 99.78%
Catalog No. T1242Cas No. 156053-89-3
Alvimopan (LY 246736) is a synthetic trans-3, 4-dimethyl-4-(3-hydroxyphenyl) piperidine with peripherally selective opioid mu receptor antagonist activity. Alvimopan is a selective and competitive antagonist at mu-opioid receptors, found in myenteric and submucosal neurons and the immune cells of the lamina propria in the human gut. Upon administration, this agent binds to mu-opioid receptors in the gut, thereby reversing opioid-related disturbances in gut motility. Alvimopan is approximately three to nine times more potent than naloxone.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$39In StockIn Stock
2 mg$55In StockIn Stock
5 mg$89In StockIn Stock
10 mg$129In StockIn Stock
25 mg$245In StockIn Stock
50 mg$396In StockIn Stock
100 mg$589In StockIn Stock
200 mg$838-In Stock
1 mL x 10 mM (in DMSO)$90In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:99.78%
Color:White
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Product Introduction

Bioactivity
Description
Alvimopan (LY 246736) is a synthetic trans-3, 4-dimethyl-4-(3-hydroxyphenyl) piperidine with peripherally selective opioid mu receptor antagonist activity. Alvimopan is a selective and competitive antagonist at mu-opioid receptors, found in myenteric and submucosal neurons and the immune cells of the lamina propria in the human gut. Upon administration, this agent binds to mu-opioid receptors in the gut, thereby reversing opioid-related disturbances in gut motility. Alvimopan is approximately three to nine times more potent than naloxone.
Targets&IC50
κ opioid receptor:40 nM(Ki), δ opioid receptor:4.4 nM, δ opioid receptor:4.4 nM(Ki), μ opioid receptor:0.77 nM(Ki)
Chemical Properties
Molecular Weight424.53
FormulaC25H32N2O4
Cas No.156053-89-3
SmilesC[C@H]1CN(C[C@H](Cc2ccccc2)C(=O)NCC(O)=O)CC[C@@]1(C)c1cccc(O)c1
Relative Density.1.166g/cm3
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 80 mg/mL (188.44 mM)
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 3.3 mg/mL (7.77 mM), Sonication is recommended.
Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.3555 mL11.7777 mL23.5555 mL117.7773 mL
5 mM0.4711 mL2.3555 mL4.7111 mL23.5555 mL
10 mM0.2356 mL1.1778 mL2.3555 mL11.7777 mL
20 mM0.1178 mL0.5889 mL1.1778 mL5.8889 mL
50 mM0.0471 mL0.2356 mL0.4711 mL2.3555 mL
100 mM0.0236 mL0.1178 mL0.2356 mL1.1778 mL

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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:
TargetMol | Animal experiments 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 DMSOTargetMol | 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 DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent 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 ddH2OTargetMol | 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.
1 Enter information below:
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2 Enter the in vivo formulation:
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