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KI3410AM-1241QuoteQuote

Chemical Characteristic

Product NameAM-1241
CAS No.444912-48-5
Molecular Weight 503.33
FormulaC22H22IN3O3
Chemical Name(2-iodo-5-nitrophenyl)-[1-[(1-methylpiperidin-2-yl)methyl]indol-3-yl]methanone
Smilesn1(cc(c2ccccc12)C(=O)c1c(ccc(c1)[N](=O)O)I)CC1N(CCCC1)C
Chemical Structure

Biological activities

AM-1241 is a selective CB2 cannabinoid receptor agonist with a Ki of 3.4 nM. AM-1241 also shows affinity for CB1 receptor with a Ki of 280 nM. AM-1241 is used for the treatment of inflammatory and neuropathic pain.[1] In [3H]CP55,940 competition binding assays, AM1241 has high affinity at the human CB2 receptor with a Ki of 7 nM. In FLIPR assays, AM-1241 blocks the agonist CP55,940-evoked Ca2+ response in a concentration dependent manner with a Kb of 63 nM.[2] AM-1241 dose-dependently reverses tactile and thermal hypersensitivity produced by ligation of the L5 and L6 spinal nerves in rats.[1] AM-1241 induces CB2-mediated antihyperalgesic effects in mice and rats. AM-1241 also stimulates the release of b-endorphin from skin keratinocytes in mice.[3] In vivo in a transgenic mouse model, AM-1241 (3.0 mg/kg) increases the survival interval after disease onset by 56%.[4]

Protocols

In vitro, AM1241 is dissolved in DMSO.[2]

References

[1] Suzuki T, et al. Pharmacological characterization of MP-412 (AV-412), a dual epidermal growth factor receptor and ErbB2 tyrosine kinase inhibitor. Cancer Sci. 2007, 98(12): 1977-1984.
[2] Suzuki T, et al. Antitumor activity of a dual epidermal growth factor receptor and ErbB2 kinase inhibitor MP-412 (AV-412) in mouse xenograft models. Cancer Sci. 2009, 100(8): 1526-1531.



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