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AM281

Alias: AM 281 AM-281 AM281
Cat No.:V9208 Purity: ≥98%
AM281 is a selective CB1 receptor blocker (antagonist) with IC50 of 9.91 nM.
AM281
AM281 Chemical Structure CAS No.: 202463-68-1
Product category: New1
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
1mg
5mg
10mg
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Product Description
AM281 is a selective CB1 receptor blocker (antagonist) with IC50 of 9.91 nM. AM281 inhibits CB2 receptors with IC50 of 13000 nM.
Biological Activity I Assay Protocols (From Reference)
ln Vitro
In SH-SY5Y cells, AM281 (0.01-10 μM) causes neurotoxicity at concentrations that raise the presence of 10 μM Aβ 25-35 when combined with 10 μM KSO 1-6 [2].
ln Vivo
Both the chronic doses of AM281 (0.62, 1.25, and 2.5 mg/kg) and the chronic doses of AM281 (2.5, 5 and 10 mg/kg) showed improvements in memory performance and exploration time [3]. The recognition index was increased to 22.1±4.8 with long-term administration of 2.5 mg/kg AM281, and memory impairment was improved to 8.5±4 with a single dosage of 5 mg/kg AM281, as opposed to 4.8±2.5 with vehicle therapy. AM281 given continuously at a dose of 2.5 mg/kg and
Animal Protocol
Animal/Disease Models: Male NMRI mice weighing 25-30 g [3] Doses: 0.62, 1.25 and 2.5 mg/kg (chronic dose); rapid dose of 5 mg/kg Can improve memory[3]. 2.5, 5 and 10 mg/kg (acute administration) Dosing: intraperitoneally (ip) (ip) with morphine daily except on the day of the experiment (chronic administration); alone 40 minutes before the second test (acute administration)
Experimental Results: Coadministration of AM281 and morphine daily Dramatically shortened exploration time compared to morphine-dependent mice receiving vehicle. The acute administration dose is 5 mg/kg, and the recognition index is Dramatically enhanced.
References

[1]. Development and preliminary validation of a plate-based CB1/CB2 receptor functional assay. Anal Biochem. 2013 Jun 15;437(2):138-43.

[2]. Effects of the CB1 cannabinoid receptor antagonist AM281 on kissorphin protection against amyloid-β neurotoxicity.

[3]. The effect of AM281, a cannabinoid antagonist, on memory performance during spontaneous morphine withdrawal in mice. Res Pharm Sci. 2013 Jan;8(1):59-64.

Additional Infomation
1-(2,4-dichlorophenyl)-5-(4-iodophenyl)-4-methyl-N-(4-morpholinyl)-3-pyrazolecarboxamide is a member of pyrazoles and a ring assembly.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C21H19N4O2CL2I
Molecular Weight
557.21116
Exact Mass
555.993
CAS #
202463-68-1
PubChem CID
4302962
Appearance
White to light yellow solid powder
Hydrogen Bond Donor Count
1
Hydrogen Bond Acceptor Count
4
Rotatable Bond Count
4
Heavy Atom Count
30
Complexity
589
Defined Atom Stereocenter Count
0
SMILES
CC1=C(N(N=C1C(NN2CCOCC2)=O)C3=C(Cl)C=C(Cl)C=C3)C4=CC=C(I)C=C4
InChi Key
AJFFBPZYXRNAIC-UHFFFAOYSA-N
InChi Code
InChI=1S/C21H19Cl2IN4O2/c1-13-19(21(29)26-27-8-10-30-11-9-27)25-28(18-7-4-15(22)12-17(18)23)20(13)14-2-5-16(24)6-3-14/h2-7,12H,8-11H2,1H3,(H,26,29)
Chemical Name
1-(2,4-dichlorophenyl)-5-(4-iodophenyl)-4-methyl-N-morpholin-4-ylpyrazole-3-carboxamide
Synonyms
AM 281 AM-281 AM281
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO : ~7.14 mg/mL (~12.81 mM)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 0.71 mg/mL (1.27 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 7.1 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 1.7947 mL 8.9733 mL 17.9466 mL
5 mM 0.3589 mL 1.7947 mL 3.5893 mL
10 mM 0.1795 mL 0.8973 mL 1.7947 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

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An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
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  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
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g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
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  • Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

Biological Data
  • Effect of acute administration of AM281 on duration of T1 (time required to achieve 20 s of object exploration) during spontaneous morphine withdrawal in all groups (n=6). Results are expressed as mean ± S.E.M. ***P<0.001, **P<0.01 and *P<0.05 in comparison to normal saline, #P<0.05 in comparison to vehicle.[3]. G Vaseghi, et al. The effect of AM281, a cannabinoid antagonist, on memory performance during spontaneous morphine withdrawal in mice. Res Pharm Sci. 2013 Jan;8(1):59-64.
  • Effect of acute administration of AM281 on memory performance on two trial object recognition task, during spontaneous morphine withdrawal. In all groups (n=6). ***P<0.001 in comparison to normal saline, #P<0.05 in comparison to vehicle.[3]. G Vaseghi, et al. The effect of AM281, a cannabinoid antagonist, on memory performance during spontaneous morphine withdrawal in mice. Res Pharm Sci. 2013 Jan;8(1):59-64.
  • Effect of chronic administration of AM281 on duration of T1 (time required to achieve 20 s of object exploration in the first trial) in morphine dependent mice. In all vehicle groups n=6. Results are expressed as mean ± S.E.M. ***P<0.001 and *P<0.05 in comparison to normal saline, #P< 0.05 in comparison to vehicle.[3]. G Vaseghi, et al. The effect of AM281, a cannabinoid antagonist, on memory performance during spontaneous morphine withdrawal in mice. Res Pharm Sci. 2013 Jan;8(1):59-64.
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