1. GPCR/G Protein Neuronal Signaling
  2. Cannabinoid Receptor
  3. AM281

AM281 

Cat. No.: HY-13505 Purity: 98.60%
COA Handling Instructions

AM281 is a selective CB1 receptor antagonist with an IC50 of 9.91 nM. AM281 inhibits CB2 receptor with an IC50 of 13000 nM.

For research use only. We do not sell to patients.

AM281 Chemical Structure

AM281 Chemical Structure

CAS No. : 202463-68-1

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1 mg USD 104 In-stock
5 mg USD 220 In-stock
10 mg USD 350 In-stock
25 mg USD 700 In-stock
50 mg USD 1100 In-stock
100 mg USD 1750 In-stock
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Description

AM281 is a selective CB1 receptor antagonist with an IC50 of 9.91 nM. AM281 inhibits CB2 receptor with an IC50 of 13000 nM[1].

IC50 & Target[1]

CB1

9.91 nM (IC50)

CB2

13000 nM (IC50)

In Vitro

AM281 (0.01-10 μM) promotes a concentration dependent increase in 10 μM Aβ 25-35 induced neurotoxicity in SH-SY5Y cells in the presence of 10 μM KSO 1-6[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Acute administration (2.5, 5 and 10 mg/kg) of AM281 shortens exploration time and improves memory performance, as does chronic administration (0.62, 1.25 and 2.5 mg/kg) of AM281[3].
Chronic administration of AM281 at 2.5 mg/kg improves recognition index to the 22.1±4.8 and single dose of AM281 at 5 mg/kg improves the memory impairment to the 8.5±4, as compared with vehicle-treated which is 4.8±2.5. Administration of AM281 at a dose of 2.5 mg/kg in chronic form and 5 mg/kg in acute dose improve memory[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male NMRI mice with the weight of 25-30 g[3]
Dosage: 0.62, 1.25 and 2.5 mg/kg (chronic administration); 2.5, 5 and 10 mg/kg (acute administration)
Administration: Administrated i.p. every day concurrently with morphine except the day of experiment (chronic administration); Singly injected 40 min before second trial (acute administration)
Result: The simultaneous daily administration of AM281 with morphine significantly shortened the exploration time, as compared with morphine-dependent mice receiving vehicle.
Acute administration at a dose of 5 mg/kg, significantly augmented recognition index.
Molecular Weight

557.21

Appearance

Solid

Formula

C21H19Cl2IN4O2

CAS No.
SMILES

O=C(C1=NN(C2=CC=C(Cl)C=C2Cl)C(C3=CC=C(I)C=C3)=C1C)NN4CCOCC4

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 7.14 mg/mL (12.81 mM; ultrasonic and warming and heat to 60°C)

Preparing
Stock Solutions
Concentration Solvent Mass 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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 0.71 mg/mL (1.27 mM); Clear solution

*All of the co-solvents are available by MedChemExpress (MCE).
Purity & Documentation

Purity: ≥99.0%

References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
AM281
Cat. No.:
HY-13505
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