An agonist of TrkB (IC50 = 47 nM in a fluorescence anisotropy assay); selectively inhibits BDNF binding to 3T3 cells expressing TrkB over those expressing TrkA

LM22A-4 – 25 mg

Brand:
Cayman
CAS:
37988-18-4
Storage:
-20
UN-No:
Non-Hazardous - /

LM22A-4 is a brain-derived neurotrophic factor (BDNF) mimetic and agonist of the receptor tropomyosin-related kinase B (TrkB; IC50 = 47 nM in a fluorescence anisotropy assay).{38767} It selectively inhibits BDNF binding to 3T3 cells expressing TrkB over those expressing TrkA, TrkC, or p75NTR. In vitro, LM22A-4 increases survival of hippocampal neurons via activation of TrkB as well as Akt and ERK downstream pro-survival signaling pathways. In vivo, LM22A-4 increases dwell time in an accelerating rotarod task, indicating improved motor learning in a rat model of traumatic brain injury. LM22A-4 restores TrkB phosphorylation in the medulla and pons and breathing frequency to wild-type levels in a mouse model of Rett syndrome when administered at a dose of 50 mg/kg.{38768} It reduces neurite degeneration, formation of intranuclear huntingtin aggregates, and improves downward climbing and grip strength in mouse models of Huntington’s disease.{38769} LM22A-4 (0.22 mg/kg) also improves limb swing speed and accelerates return to normal gait accuracy in a mouse model of hypoxic-ischemic stroke.{38770}  

 

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Description

An agonist of TrkB (IC50 = 47 nM in a fluorescence anisotropy assay); selectively inhibits BDNF binding to 3T3 cells expressing TrkB over those expressing TrkA, TrkC, or p75NTR; increases survival of hippocampal neurons in vitro, restores neurogenesis and improves cognitive deficits in mouse models of ischemic stroke, Huntington’s disease, Rett syndrome, and a rat model of traumatic brain injury,

Formal name: N1,N3,N5-tris(2-hydroxyethyl)-1,3,5-benzenetricarboxamide

Synonyms: 

Molecular weight: 339.3

CAS: 37988-18-4

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Activators|Kinases||Research Area|Neuroscience|Behavioral Neuroscience|Learning & Memory||Research Area|Neuroscience|Neurodegenerative Disorders|Huntington’s Disease

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