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AM281

Name: AM281
Brand: TargetMol
SKU: T2264
Price: 77 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T2264Cas No. 202463-68-1

AM 281, a cannabinoid antagonist, reduces neurologic dysfunction and mortality rate after cecal ligation and puncture in rats.

AM281

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Purity: 99.76

Catalog No. T2264Cas No. 202463-68-1

AM 281, a cannabinoid antagonist, reduces neurologic dysfunction and mortality rate after cecal ligation and puncture in rats.

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$77	In Stock	In Stock
5 mg	$182	In Stock	In Stock
10 mg	$288	In Stock	In Stock
25 mg	$582	In Stock	In Stock
50 mg	$833	In Stock	In Stock
100 mg	$1,150	In Stock	In Stock
500 mg	$2,290	-	In Stock
1 mL x 10 mM (in DMSO)	$258	In Stock	In Stock

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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.

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:99.76

Color:White

Resource Download

COA HNMR LCMS

Product Introduction

AM281 AI Summary

AM281 exhibits high affinity for the cannabinoid CB1 receptor, acting as both an inverse agonist and antagonist, with a Ki value ranging from 4.5 nM to 422.0 nM depending on the assay system used. It demonstrates significantly lower affinity for the CB2 receptor, with a Ki value of 4200.0 nM. In various cellular assays, AM281 shows broad bioactivity, including inhibition of Menin-MLL interaction, Jumonji Domain 2E, Tyrosyl-DNA Phosphodiesterase (TDP1), several cytochrome P450 enzymes (2C19, 2D6, 2C9), Tau fibril formation, 15-human lipoxygenase, Anthrax lethal toxin internalization, lipid storage modulation, Regulator of G Protein Signaling 4, and USP1/UAF1. It also exhibits antagonist activity at the CB1 receptor with negative intrinsic activity levels of -80.0% and -42.0% in human recombinant and rat brain cortical membranes, respectively, and agonist activity at the human GPR55 receptor (EC50 = 13600.0 nM). Additionally, AM281 has antiviral properties, inhibiting SARS-CoV-2 induced cytotoxicity in Caco-2 and VERO-6 cells at 10 µM concentration. It possesses mild inhibition of the SARS-CoV-2 3CL-Pro protease (21.46% at 20 µM) and exhibits minimal inhibition of the human HDAC6 enzyme. The compound also has a distribution coefficient with a CLogD value of 3.71. Overall, AM281 displays a diverse range of bioactivities, including enzyme inhibition, receptor modulation, and antiviral effects..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description	AM 281, a cannabinoid antagonist, reduces neurologic dysfunction and mortality rate after cecal ligation and puncture in rats.
Targets&IC50	CB2:13000 nM (IC50), CB1:9.91 nM (IC50)

Chemical Properties

Molecular Weight	557.21
Formula	C₂₁H₁₉Cl₂IN₄O₂
Cas No.	202463-68-1
Smiles	CC1=C(N(N=C1C(NN2CCOCC2)=O)C3=C(Cl)C=C(Cl)C=C3)C4=CC=C(I)C=C4
Relative Density.	1.7g/cm3

Storage & Solubility Information

Storage

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

Solubility Information

DMSO: 12 mg/mL (21.54 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+90% Corn Oil: 0.5 mg/mL (0.9 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

	1mg	5mg	10mg	50mg
1 mM	1.7947 mL	8.9733 mL	17.9466 mL	89.7328 mL
5 mM	0.3589 mL	1.7947 mL	3.5893 mL	17.9466 mL
10 mM	0.1795 mL	0.8973 mL	1.7947 mL	8.9733 mL
20 mM	0.0897 mL	0.4487 mL	0.8973 mL	4.4866 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