LM22A-4 - Trk Receptor Agonist - 生命科学试剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemELM22A-4Cat. No.: HY-100673CAS No.: 37988-18-4分式: CHNO分量: 339.34作靶点: Trk Receptor作通路: Neuronal Signaling; Protein Tyrosine Kinase/RTK储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 H2O : 50 mg/mL (

2、147.34 mM)DMSO : 29 mg/mL (85.46 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.9469 mL 14.7345 mL 29.4690 mL5 mM 0.5894 mL 2.9469 mL 5.8938 mL10 mM 0.2947 mL 1.4734 mL 2.9469 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。体内实验请根据您的实验动物和给药式选择适当的溶解案，配制前

3、请先配制澄清的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的作液，建议您现现配，当天使；澄清的储备液可以根据储存条件，适当保存；以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (7.37 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (7.37 mM); Clear solution1/3

4、 Master of Small Molecules 您边的抑制剂师www.MedChemE3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (7.37 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 LM22A-4种特异性的 tyrosine kinase receptor B 激动剂，常于神经系统疾病研究。体外研究 LM22A-4 significantly up-regulates OPN and ALPase mRNA expression in a dose-dependent man

5、ner andOC mRNA level is significantly increased by 5 M of LM22A-4. LM22A-4 significantly increases OPN,ALPase and OC mRNA expression in a time-dependent manner. LM22A-4 stimulated OPN and OC mRNAexpression in HCEM cells cultured with mineralizing media 2.体内研究 LM22A-4 (10 mg/kg, i.p.) significantly r

6、educes the degree of tissue injury and apoptosis (TUNEL staining andcaspase-3 and Bcl-2 expression) compared with vehicle treated group. LM22A-4 also significantlyameliorates the recovery of limb function. LM22A-4 (10 mg/kg) treatment results in a significant increase inneuron number. LM22A-4 admini

7、stration (10 mg/kg) significantly improves the neurological scores comparedwith those of the solvent-treated animals 1.PROTOCOLAnimal ICR mice are randomly divided into five groups: sham treatment, spinal cord injury, spinal cord injuryAdministration 1 combined with solvent treatment, spinal cord in

8、jury combined with LM22A-4 treatment (10 mg/kg), and spinalcord injury combined with LM22A-4 treatment (15 mg/kg), with each group containing 26 animals.Preparation of the mouse SCI model is based on a previous study and on a protocol employed by this group.Briefly, a mouse is anesthetized via the a

9、dministration of chloral hydrate (4 mg/kg) before a 3-cm incision isintroduced on its back. T7-T11 vertebrae are exposed under a surgical microscope before the laminae areremoved with a vascular clip to fully expose the spinal cord. The spinal cord is clamped with the vascular clipfor 1 minute with

10、a force of 10 g. The animal is then subjected to complete staunching of the bleeding, andthe incised dorsal muscle and skin are sutured. Mice from the control group undergo laminectomy, fullexposure of the spinal cord, and subsequent suturing, but without aortic clamping. After the surgery, the mice

11、are placed on a warm blanket until fully awake and are then housed in cages accommodating a normal diet.After the SCI treatment, 14 mice are sacrificed to enable molecular and histological examinations; the other14 mice are allowed to live for 20 days for neurological scoring and are sacrificed on d

12、ay 20 via cervicaldislocation.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Yu G, et al. Protective effects of LM22A-4 on injured spinal cord nerves. Int J Clin Exp Pathol. 2015 Jun 1;8(6):6526-32. eCollection2015.2. Kajiya M, et al. BDNF mimetic compound LM22A-4 regulates cementoblast differentiation via the TrkB-ERK/Akt signaling cascade. IntImmunopharmacol. 2014 Apr;19(2):245-52.2/3 Master of Small Molecules 您边的抑制剂师www.MedChemEMcePdfHeight