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CAS No. : 342777-54-2
|Size||Stock||Price||Quantity||Add to Cart||Quotation Online|
|2mg||In-stock||USD 120.0 120.0|
|5mg||In-stock||USD 180.0 180.0|
|10mg||In-stock||USD 300.0 300.0|
|50mg||In-stock||USD 1092.0 1092.0|
|100mg||In-stock||USD 1920.0 1920.0|
|Cat. No. :||CS-7663|
|CAS No. :||342777-54-2|
|M. Wt. :||485.01|
|Solubility:||DMSO: ≥ 150 mg/mL|
LM22B-10 is an activator of TrkB/TrkC neurotrophin receptor, and can induce TrkB, TrkC, AKT and ERK activation in vitro and in vivo. In Vitro: LM22B-10 exhibits maximum neurotrophic survival activity levels that are higher than those maximally achieved with BDNF (53 ± 7.2% above BDNF at 0.7 nM) and NT-3 (91 ± 8.6% above NT-3 at 0.7 nM) with an EC50 value of 200-300 nM. LM22B-10 (1000 nM) induces neurites of significantly larger average lengths, up to -40 μM. LM22B-10 (250-2000 nM) binds to TrkB-Fc and TrkC-Fc in a dose-dependent manner. LM22B-10 inhibits binding of BDNF to TrkB-expressing cells and NT-3 to TrkC-expressing cells. LM22B-10 promotes cell survival and functions preferentially through TrkB and TrkC. LM22B-10, but not BDNF or NT-3, promotes neurite outgrowth in an inhibitory environment. LM22B-10 induces patterns of Trk and downstream signaling activation that are distinct from those of BDNF and NT-3. LM22B-10 also induces TrkB, TrkC, AKT and ERK activation in hippocampal neurons in culture. In Vivo: LM22B-10 (0.5 mg/kg) activates TrkB, TrkC, AKT and ERK in C57BL/6J mice. LM22B-10 (50 mg/kg, i,p,) shows increased phosphorylation at TrkBY817 and TrkCY820. LM22B-10 activates synaptic TrkB and TrkC and increases pre- and post-synaptic proteins and spine density in aged mice.
Protocol:Cell Assay: LM22B-10 is dissolved in 0.04 N HCl prior to dilution (1:10,000) in culture medium.Mouse NIH-3T3 cells, mouse NIH-3T3 cells expressing TrkA (NIH-3T3-TrkA) or p75NTR (NIH-3T3-p75NTR), and NIH-3T3 cells expressing TrkB (NIH-3T3-TrkB) or TrkC (NIH-3T3-TrkC) are propagated in DMEM supplemented with 10% FBS and 200-400 μg/mL Geneticin (for Trk-expressing cells) or 400 μg/mL hygromycin (for p75NTR-expressing cells). Cells are seeded into 24-well plates (30,000 cells/well) and cultured in medium consisting of 50% PBS and 50% DMEM without supplements. Following exposure to growth factors (0.7 nM) or 1000 nM LM22B-10 for 72-96 h, cells are suspended in 50 μL lysis buffer, transferred to opaque 96-well culture plates and survival is measured using the ViaLight Assay.
Yang T, et al. A small molecule TrkB/TrkC neurotrophin receptor co-activator with distinctive effects on neuronal survival and process outgrowth. Neuropharmacology. 2016 Nov;110(Pt A):343-61.
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