ML352 是一种突触前胆碱转运蛋白 (CHT) 的非竞争性抑制剂,对表达人 CHT 和小鼠前脑突触体的 HEK293 细胞的 Kivalue 分别为 92 和 166 nM。
Cas No. | 1649450-12-3 |
化学名 | (Z)-N-((3-isopropylisoxazol-5-yl)methyl)-4-methoxy-3-((1-methylpiperidin-4-yl)oxy)benzimidic acid |
Canonical SMILES | CC(C1=NOC(C/N=C(O)/C2=CC(OC(CC3)CCN3C)=C(OC)C=C2)=C1)C |
分子式 | C21H29N3O4 |
分子量 | 387.47 |
溶解度 | 5mg/mL in ethanol, 20mg/mL in DMSO or DMF |
储存条件 | Store at -20℃ |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
产品描述 | ML-352 is a noncompetitive inhibitor of the presynaptic choline transporter (CHT) with Ki values of 92 and 166 nM for HEK293 cells expressing human CHT and mouse forebrain synaptosomes, respectively.[1] It is selective for CHT over dopamine, norepinephrine, and serotonin transporters in HEK293 cells expressing human transporters when used at a concentration of 5 μM as well as a panel of 68 G protein-coupled receptors, ion channels, and transporters when used at a concentration of 10 μM. ML-352 (5 μM) increases cell surface expression of CHT without affecting total protein levels. Reference: [1]. Ennis, E.A., Wright, J., Retzlaff, C.L., et al. Identification and characterization of ML352: A novel, noncompetitive inhibitor of the presynaptic choline transporter. ACS Chem. Neurosci. 6(3), 417-427 (2015). |