LM22B-10-DataSheet-生命科學(xué)試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemELM22B-10Cat. No.: HY-104047CAS No.: 342777-54-2分式: CHClNO分量: 485.01作靶點(diǎn): Trk Receptor; Akt; ERK作通路: Neuronal Signaling; Protein Tyrosine Kinase/RTK;PI3K/Akt/mTOR; MAPK/ERK Pathway; Stem Cell/Wnt儲存式: Powder -20C 3 years4C 2 yearsI

2、n solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 150 mg/mL (309.27 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 2.0618 mL 10.3091 mL 20.6181 mL5 mM 0.4124 mL 2.0618 mL 4.1236 mL10 mM 0.2062 mL 1.0309 mL 2.0618 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液

3、的保存式和期限。體內(nèi)實(shí)驗(yàn)請根據(jù)您的實(shí)驗(yàn)動物和給藥式選擇適當(dāng)?shù)娜芙獍福渲魄罢埾扰渲瞥蔚膬湟?，再依次添加助溶?為保證實(shí)驗(yàn)結(jié)果的可靠性，體內(nèi)實(shí)驗(yàn)的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使；澄的儲備液可以根據(jù)儲存條件，適當(dāng)保存；以下溶劑前的百分指該溶劑在您配制終溶液中的體積占)：1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (5.15 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5

4、mg/mL (5.15 mM); Clear solution1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemE3. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (5.15 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 LM22B-10種 TrkB/TrkC 神經(jīng)營養(yǎng)因受體激活劑，能夠誘導(dǎo)體內(nèi)體外 TrkB，TrkC，AKT 和 ERK 的活化。IC50 & Target TrkB TrkC Akt ERK體外研究 LM22B-10 exhibi

5、ts maximum neurotrophic survival activity levels that are higher than those maximallyachieved 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 anEC50 value of 200-300 nM. LM22B-10 (1000 nM) induces neurites of significantly larger average lengths, upto -40 M. LM2

6、2B-10 (250-2000 nM) binds to TrkB-Fc and TrkC-Fc in a dose-dependent manner. LM22B-10inhibits binding of BDNF to TrkB-expressing cells and NT-3 to TrkC-expressing cells. LM22B-10 promotescell survival and functions preferentially through TrkB and TrkC. LM22B-10, but not BDNF or NT-3, promotesneurite

7、 outgrowth in an inhibitory environment. LM22B-10 induces patterns of Trk and downstream signalingactivation that are distinct from those of BDNF and NT-3. LM22B-10 also induces TrkB, TrkC, AKT and ERKactivation in hippocampal neurons in culture 1.體內(nèi)研究 LM22B-10 (0.5 mg/kg) activates TrkB, TrkC, AKT

8、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 TrkCand increases pre- and post-synaptic proteins and spine density in aged mice 1.PROTOCOLCell Assay 1 Mouse NIH-3T3 cells, mouse NIH-3T3 cells expressin

9、g 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 DMEMsupplemented with 10% FBS and 200-400 g/mL Geneticin (for Trk-expressing cells) or 400 g/mLhygromycin (for p75NTR-expressing cells). Cells are seeded into 24

10、-well plates (30,000 cells/well) andcultured in medium consisting of 50% PBS and 50% DMEM without supplements. Following exposure togrowth factors (0.7 nM) or 1000 nM LM22B-10 for 72-96 h, cells are suspended in 50 L lysis buffer,transferred to opaque 96-well culture plates and survival is measured

11、using the ViaLight Assay.MCE has not independently confirmed the accuracy of these methods. They are for reference only. Asian Pac J Trop Med. 2017 Dec;10(12):1172-1176.See more customer validations on HYPERLINK / www.MedChemEREFERENCES2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemE1. Yang T, et al. A small molecule TrkB/TrkC neurotrophin receptor co-activator with distinctive effects on neuronal survival and processoutgrowth. Neuropharmacology. 2016 Nov;110(Pt A):343-61.McePdfHeightCaution: Product