An agonist of TrkB
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LM22A-4

Item No. 22082

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N1,N3,N5-tris(2-hydroxyethyl)-1,3,5-benzenetricarboxamide
CAS Number
37988-18-4
Molecular Formula
C15H21N3O6
Formula Weight
339.3
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 10 mg/mlDMSO: 30 mg/mlPBS (pH 7.2): 10 mg/ml
SMILES
O=C(NCCO)C1=CC(C(NCCO)=O)=CC(C(NCCO)=O)=C1
InChi Code
InChI=1S/C15H21N3O6/c19-4-1-16-13(22)10-7-11(14(23)17-2-5-20)9-12(8-10)15(24)18-3-6-21/h7-9,19-21H,1-6H2,(H,16,22)(H,17,23)(H,18,24)
InChi Key
RGWJKANXFYJKHN-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $69

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    10 mg

    $120

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    25 mg

    $280

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    50 mg

    $525

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    Product Description

    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).1 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.2 It reduces neurite degeneration, formation of intranuclear huntingtin aggregates, and improves downward climbing and grip strength in mouse models of Huntington's disease.3 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.4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Massa, S.M., Yang, T., Xie, Y., et al. Small molecule BDNF mimetics activate TrkB signaling and prevent neuronal degeneration in rodents. J. Clin. Invest. 120(5), 1774-1785 (2010).

    2. Schmid, D.A., Yang, T., Ogier, M., et al. A TrkB small molecule partial agonist rescues TrkB phosphorylation deficits and improves respiratory function in a mouse model of Rett syndrome. J. Neurosci. 32(5), 1803-1810 (2012).

    3. Simmons, D.A., Belichenko, N.P., Yang, T., et al. A small molecule TrkB ligand reduces motor impairment and neuropathology in R6/2 and BACHD mouse models of Huntington’s disease. J. Neurosci. 33(48), 18712-18727 (2013).

    4. Han, J., Pollak, J., Yang, T., et al. Delayed administration of a small molecule tropomyosin-related kinase B ligand promotes recovery after hypoxic-ischemic stroke. Stroke 43(7), 1918-1924 (2012).