S89446 |
WAY-213613 hydrochloride |
源叶(MedMol) | 98% |
- 产品描述: WAY-213613 is a potent and selective human EAAT2 inhibitor. WAY-213613 has potent EAAT2 inhibitory activity with an IC50 value of 85 nM. WAY-213613 can be used for the research of central nervous system
- 靶点: EAAT2;transporter
- 体外研究:
WAY-213613 (0-100 μM) has inhibitory activity for human EAAT1, EAAT2 and EAAT3 subtype with IC50 values of 5004 nM, 85 nM and 3787 nM, respectively. WAY-213613 (3, 30, 300 nM) has the inhibitory effect on synaptosomal L-[3H] glutamate uptake with Ki values of 15 nM, 41 nM and 55 nM in the presence of 3, 30 and 300 nM, respectively. WAY-213613 (0-100 μM) produces a concentration-dependent block of glutamate-induced currents in EAAT1-, EAAT2- or EAAT3-injected oocytes, with IC50 values of 48, 0.13 and 4.0 μM, respectively. WAY-213613 (0.5–50 μM) exhibits good selectivity over ionotropic receptors and EAAT2 and potent activity toward blocking NMDA-stimulated responses
- 参考文献:
1. Dunlop J, et al. Characterization of novel aryl-ether, biaryl, and fluorene aspartic acid and diaminopropionic acid analogs as potent inhibitors of the high-affinity glutamate transporter EAAT2. Mol Pharmacol. 2005 Oct;68(4):974-82. Epub 2005 Jul 13. 2. Simmons DA, et al. A small molecule p75NTR ligand, LM11A-31, reverses cholinergic neurite dystrophy in Alzheimer's disease mouse models with mid- to late-stage disease progression. PLoS One. 2014 Aug 25;9(8):e102136.
- 保存条件: -20℃
- 配置溶液浓度参考:
1mg 5mg 10mg 1 mM 2.214 ml 11.071 ml 22.141 ml 5 mM 0.443 ml 2.214 ml 4.428 ml 10 mM 0.221 ml 1.107 ml 2.214 ml 50 mM 0.044 ml 0.221 ml 0.443 ml
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