ML352
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
神经递质乙酰胆碱(ACh)在自主功能\运动控制\注意力\学习与记忆以及奖励中起着关键作用.高亲和力的胆碱转运体(CHT)是乙酰胆碱合成的限速因素,但CHT在突触胆碱信号检测与调控方面的应用仍有待开发.ML352是新型的非竞争性突触前胆碱转运体抑制剂.
体外:在转染细胞与神经末梢制备物中,ML352在完全拮抗CHT的浓度下对乙酰胆碱酯酶或胆碱乙酰转移酶无抑制作用,也缺乏对多巴胺\血清素\去甲肾上腺素转运体\多种受体以及离子通道的活性.ML352呈非竞争性地抑制完整细胞摄取胆碱并减少膜试验中密胆碱3结合位点的表观密度,这提示ML352与转运体之间的变构相互作用[1].
体内:DMPK实验表明,ML352具有较高的静脉血浆清除率.此外,药物口服生物利用度以及脑内总浓度表明,ML352有望作为一种合适的探针,用于研究啮齿动物体内可变的乙酰胆碱信号以及行为学效应[2].
临床试验:到目前为止,ML352还处于临床前开发阶段.
参考文献:
[1] Ennis EA, Wright J, Retzlaff CL, McManus OB, Lin Z, Huang X, Wu M, Li M, Daniels JS, Lindsley CW, Hopkins CR, Blakely RD. Identification and characterization of ML352: a novel, noncompetitive inhibitor of the presynaptic choline transporter. ACS Chem Neurosci. 2015 Mar 18;6(3):417-27.
[2] Elizabeth Ennis Miss, Jane Wright, James Tarr, Charles Locuson, Corey Hopkins, J Daniels, Craig Lindsley and Randy Blakely. A Novel Approach to Cholinergic Signaling Modulation: Development and Characterization of ML352, a Novel, Noncompetitive Inhibitor of the Presynaptic Choline Transporter. The FASEB Journal vol. 29 no. 1 Supplement 932.6
Storage | Store at -20°C |
M.Wt | 387.47 |
Cas No. | 1649450-12-3 |
Formula | C21H29N3O4 |
Solubility | Soluble in DMSO |
Chemical Name | (Z)-N-((3-isopropylisoxazol-5-yl)methyl)-4-methoxy-3-((1-methylpiperidin-4-yl)oxy)benzimidic acid |
SDF | Download SDF |
Canonical SMILES | CC(C1=NOC(C/N=C(O)/C2=CC(OC(CC3)CCN3C)=C(OC)C=C2)=C1)C |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |