LEI-401
目录号: PL09749 纯度: ≥99%
CAS No. :2393840-15-6
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中文名称
LEI-401
英文名称
LEI-401
英文别名
YW2065;CC1=C(C=NN1C1=C(Br)C=CC=C1)C(=O)NC1=NC2=CC=CC=C2C=C1;1-(2-Bromophenyl)-5-methyl-N-(quinolin-2-yl)-1H-pyrazole-4-carboxamide;1H-Pyrazole-4-carboxamide, 1-(2-bromophenyl)-5-methyl-N-2-quinolinyl-;1H-aPyrazole-a?-acarboxamide, 1-a?2-abromophenyl)a?a?-amethyl-aN-a?-aquinolinyl-;Schembl20604119;LEI-401
Cas No.
2393840-15-6
分子式
C20H15BrN4O
分子量
407.26
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
LEI-401 是一种首创的、选择性的、通过血脑屏障的 NAPE-PLD (N-酰基磷酰乙醇胺磷脂酶 D) 抑制剂,IC50 为 27 nM。LEI-401 对小鼠情绪行为的调节。
生物活性
LEI-401 is a first-in-class, selective, and CNS-active NAPE-PLD (N-acylphosphatidylethanolamine phospholipase D) inhibitor, with an IC 50 of 27 nM. LEI-401 modulates emotional behavior in mice.
性状
Solid
体外研究(In Vitro)
LEI-401 reduced a broad range of NAEs including anandamide in neuronal cells in a NAPE-PLD-dependent manner. LEI-401 (0.04-20 μM; 30?minutes) dose-dependently reduces the labeling of NAPE-PLD with an IC50 of 0.86 μM in hNAPE-PLD-transfected HEK293T cells. LEI-401 reduces NAE levels in Neuro-2a cells, but not in NAPE-PLD KO cells. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
LEI-401 (30?mg/kg; i.p.) diminishes fear extinction in mice.
LEI-401 also activates HPA axis signaling.
LEI-401 (10 mg/kg; p.o.) treatment shows the t 1/2 , C max , t max , AUC last , and F values of 2.5 hours, 1370 ng/mL, 2 hours, 6760 h*ng/mL, and 25%, respectively.
LEI-401 (30 mg/kg; i.p.) treatment show the C max , t max , AUC last , and F values of 10300 ng/mL, 1 hour, 38600 h*ng/mL, and 48%, respectively. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Mock ED, et al. Discovery of a NAPE-PLD inhibitor that modulates emotional behavior in mice. Nat Chem Biol. 2020;16(6):667-675.
溶解度数据
In Vitro: DMSO : 100 mg/mL (237.23 mM; Need ultrasonic)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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