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ML352

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Chemical Structure| 1649450-12-3 同义名 : -
CAS号 : 1649450-12-3
货号 : A198263
分子式 : C21H29N3O4
纯度 : 97%
分子量 : 387.473
MDL号 : MFCD28975158
存储条件:

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 250 mg/mL(645.21 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方:
生物活性
描述 The high-affinity choline transporter (CHT) is the rate-limiting determinant of acetylcholine (ACh) synthesis, yet the transporter remains a largely undeveloped target for the detection and manipulation of synaptic cholinergic signaling. ML352 is a selective CHT inhibitor. ML352 inhibited [3H]choline uptake with high affinity (Ki = 92 ± 2.8 nM). When combined with fixed concentrations of ML352, a concentration-dependent reduction in transport Vmax relative to vehicle-treated control was evident (Vmax 200 nM ML352 = 70.4 ± 5.6%; 800 nM, 30.3 ± 4.2%). Analysis of ML352 inhibitory actions on choline uptake in mouse forebrain synaptosomes yielded similar effects (Vmax 300 nM ML352 = 57.2 ± 3.4%). ML352 demonstrated dose-dependent inhibition of HC-3 binding, well-fit by a single-site inhibition model (r = 0.948) with a Ki of 128.6 ± 15.3 nM, similar to that found in uptake inhibition studies. In support of uptake inhibition findings, a significant reductions in [3H]HC-3 binding Bmax (Bmax 200 nM ML352 = 80.3 ± 3.8%; 800 nM, 48.9 ± 4.1%) was observed. ML352 at saturating concentrations (5 μM) also induced a significant increase in hCHT surface expression (43.4 ± 4.7% of control)[1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.58mL

0.52mL

0.26mL

12.90mL

2.58mL

1.29mL

25.81mL

5.16mL

2.58mL

参考文献

[1]Ennis EA, Wright J, Retzlaff CL, et al. Identification and characterization of ML352: a novel, noncompetitive inhibitor of the presynaptic choline transporter. ACS Chem Neurosci. 2015;6(3):417-427