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LM11A-31 dihydrochloride

Names

[ CAS No. ]:
1243259-19-9

[ Name ]:
LM11A-31 dihydrochloride

[Synonym ]:
(2S,3S)-2-amino-3-methyl-N-(2-morpholin-4-ylethyl)pentanamide

Biological Activity

[Description]:

LM11A-31 dihydrochloride, a p75NTR (neurotrophin receptor p75) Ligand, is a potent proNGF (nerve growth factor) antagonist. LM11A-31 dihydrochloride is a water-soluble, non-peptide with high blood-brain barrier permeability[1][2].

[Related Catalog]:

Signaling Pathways >> Others >> Others

[Target]

proNGF[1]


[In Vivo]

LM11A-31 (oral gavage; 50 mg kg/day for 4 weeks) significantly mitigates proNGF accumulation and preserves BRB integrity[1]. LM11A-31 (orally; 50 or 75 mg/kg) administered for 3 months starting at 6-8 months of age prevents and/or reverses atrophy of basal forebrain cholinergic neurites and cortical dystrophic neurites in mid-stage male APPL/S mice[2]. Animal Model: Male C57BL/6 J mice[1] Dosage: 50 mg kg/day Administration: Oral gavage; for 4 weeks Result: Mitigated proNGF accumulation and preserved BRB integrity.

[References]

[1]. Elshaer SL, et al. Modulation of the p75 neurotrophin receptor using LM11A-31 prevents diabetes-induced retinalvascular permeability in mice via inhibition of inflammation and the RhoA kinase pathway. Diabetologia. 2019 Aug;62(8):1488-1500.

[2]. Simmons DA, et al. A small molecule p75NTR ligand, LM11A-31, reverses cholinergic neurite dystrophy in Alzheimer's disease mouse models with mid- to late-stage disease progression. PLoS One. 2014 Aug 25;9(8):e102136.

Chemical & Physical Properties

[ Molecular Formula ]:
C12H27Cl2N3O2

[ Molecular Weight ]:
243.34600

[ Exact Mass ]:
243.19500

[ PSA ]:
71.08000

[ LogP ]:
1.28670


Related Compounds