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Cat. No. Name Size Price Add Cart
KI3400Semagacestat (LY450139)QuoteQuote

Chemical Characteristic

Product NameSemagacestat (LY450139)
SynonymsLY450139
CAS No.425386-60-3
Molecular Weight 361.44
FormulaC19H27N3O4
Chemical Name(2S)-2-hydroxy-3-methyl-N-[(2S)-1-[[(5S)-3-methyl-4-oxo-2,5-dihydro-1H-3-benzazepin-5-yl]amino]-1-oxopropan-2-yl]butanamide
SmilesC(=O)([C@H](C(C)C)O)N[C@H](C(=O)NC1C(=O)N(CCc2c1cccc2)C)C
Chemical Structure

Biological activities

Semagacestat is an azepine class γ-secretase inhibitor. Semagacestat inhibits γ-secretase Ab42, Ab40 and Ab38, with IC50s of 10.9, 12.1 and 12.0 nM, respectively. Semagacestat inhibits Notch signaling with an IC50 of 14.1 nM.

Protocols

In vitro, semagacestat is dissolved in DMSO and diluted 1/10 in phosphate-buffered saline.[4]

References

[1] Ibrahim MM, et al. Activation of CB2 cannabinoid receptors by AM1241 inhibits experimental neuropathic pain: pain inhibition by receptors not present in the CNS. Proc Natl Acad Sci U S A. 2003, 100(18): 10529-10533.
[2] Yao BB, et al. In vitro pharmacological characterization of AM1241: a protean agonist at the cannabinoid CB2 receptor? Br J Pharmacol. 2006, 149(2):145-154.
[3] Guindon J, et al. Cannabinoid CB2 receptors: a therapeutic target for the treatment of inflammatory and neuropathic pain. Br J Pharmacol. 2008, 153(2): 319-334.
[4] Shoemaker JL, et al. The CB2 cannabinoid agonist AM-1241 prolongs survival in a transgenic mouse model of amyotrophic lateral sclerosis when initiated at symptom onset. J Neurochem. 2007, 101(1): 87-98.

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