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AT-121

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Catalog No. T37610Cas No. 2099681-31-7

AT-121 is a dual μ-opioid and neuropeptide receptor partial agonist (Kis 16.49 and 3.67 nM, respectively). It stimulates [35S]GTPγS binding to cell membranes expressing either μ-opioid receptors or neuropeptide receptors (EC50s of 19.6 and 34.7 nM, respectively.) AT-121 (0.003-0.03 mg/kg) reduced capsaicin-induced thermal anisocoria in a dose-dependent manner, but did not increase scratching activity in rhesus monkeys. In rhesus monkey drug self-administration tests, AT-121 at doses of 0.3 to 10 μg/kg per injection lacked reinforcing effects (a potential marker of abuse) and did not reduce the reinforcing effects of food pellets.AT-121 (0.01 or 0.03 mg/kg) did not induce hyperalgesia, a marker of tolerance, in rhesus monkeys.AT-121 is a safe non-addictive pain reliever with anti-injury and analgesic effects.

AT-121

AT-121

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Hot
Purity: 99.97%
Catalog No. T37610Cas No. 2099681-31-7
AT-121 is a dual μ-opioid and neuropeptide receptor partial agonist (Kis 16.49 and 3.67 nM, respectively). It stimulates [35S]GTPγS binding to cell membranes expressing either μ-opioid receptors or neuropeptide receptors (EC50s of 19.6 and 34.7 nM, respectively.) AT-121 (0.003-0.03 mg/kg) reduced capsaicin-induced thermal anisocoria in a dose-dependent manner, but did not increase scratching activity in rhesus monkeys. In rhesus monkey drug self-administration tests, AT-121 at doses of 0.3 to 10 μg/kg per injection lacked reinforcing effects (a potential marker of abuse) and did not reduce the reinforcing effects of food pellets.AT-121 (0.01 or 0.03 mg/kg) did not induce hyperalgesia, a marker of tolerance, in rhesus monkeys.AT-121 is a safe non-addictive pain reliever with anti-injury and analgesic effects.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$350In StockIn Stock
5 mg$828In StockIn Stock
10 mg$1,130In StockIn Stock
25 mg$1,590In StockIn Stock
50 mg$1,980In StockIn Stock
100 mg$2,500In StockIn Stock
500 mg$4,9006-8weeks6-8weeks
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
This molecule is a custom-made product. TargetMol has an excellent synthesis team with the experience and capability to provide you with cost-effective products. If you have any questions, please feel free to contact us. We are committed to serving you wholeheartedly.
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Purity:99.97%
Appearance:Solid
Color:White to Yellow
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Product Introduction

Bioactivity
Description
AT-121 is a dual μ-opioid and neuropeptide receptor partial agonist (Kis 16.49 and 3.67 nM, respectively). It stimulates [35S]GTPγS binding to cell membranes expressing either μ-opioid receptors or neuropeptide receptors (EC50s of 19.6 and 34.7 nM, respectively.) AT-121 (0.003-0.03 mg/kg) reduced capsaicin-induced thermal anisocoria in a dose-dependent manner, but did not increase scratching activity in rhesus monkeys. In rhesus monkey drug self-administration tests, AT-121 at doses of 0.3 to 10 μg/kg per injection lacked reinforcing effects (a potential marker of abuse) and did not reduce the reinforcing effects of food pellets.AT-121 (0.01 or 0.03 mg/kg) did not induce hyperalgesia, a marker of tolerance, in rhesus monkeys.AT-121 is a safe non-addictive pain reliever with anti-injury and analgesic effects.
Targets&IC50
μ opioid receptor:16.49 nM(Ki ), Nociception:3.67 nM(Ki ), [35S]-GTPγS:19.6 nM(EC50), [35S]-GTPγS:34.7 nM(EC50)
In vivo
AT-121 (0.003-0.03 mg/kg; s.c.; rhesus monkeys) decreases capsaicin-induced thermal allodynia dose-dependently without increasing scratching activity or inducing hyperalgesia, a marker of tolerance development, in doses of 0.01 or 0.03 mg/kg in rhesus monkeys. [1]
Chemical Properties
Molecular Weight462.65
FormulaC24H38N4O3S
Cas No.2099681-31-7
SmilesO=C1C2(C=3C(CN1CCNS(N)(=O)=O)=CC=CC3)CCN(CC2)[C@@H]4CC[C@H]([C@H](C)C)CC4
Relative Density.1.25 g/cm3 (Predicted)
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: 55 mg/mL (118.88 mM), Sonication is recommended.
Chloroform: 9 mg/mL (19.45 mM), Sonication is recommended.
DMF: Miscible
Ethanol: Miscible
Ethanol:PBS (pH 7.2) (1:20): 50 μg/mL, Sonication is recommended.
Solution Preparation Table
Chloroform/DMSO
1mg5mg10mg50mg
1 mM2.1615 mL10.8073 mL21.6146 mL108.0731 mL
5 mM0.4323 mL2.1615 mL4.3229 mL21.6146 mL
10 mM0.2161 mL1.0807 mL2.1615 mL10.8073 mL
DMSO
1mg5mg10mg50mg
20 mM0.1081 mL0.5404 mL1.0807 mL5.4037 mL
50 mM0.0432 mL0.2161 mL0.4323 mL2.1615 mL
100 mM0.0216 mL0.1081 mL0.2161 mL1.0807 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:
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:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

Dose Conversion

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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

Keywords

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