VU0359595|1246303-14-9|(CID-53361951; ML-270)-陌孚医药/Medlife

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VU0359595 (Synonyms: CID-53361951; ML-270)

目录号: PC12730 纯度: ≥98%

CAS No. :1246303-14-9

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PC12730-5mg	5mg	¥1890.00	请登录
PC12730-10mg	10mg	¥3406.00	请登录
PC12730-25mg	25mg	¥7669.00	请登录

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中文名称	VU0359595
英文名称	VU0359595
英文别名	VU0359595;(1R,2R)-N-([S]-1-{4-[5-Bromo-2-oxo-2,3-dihydro-1H-benzo(d)imidazol-1-yl]piperidin-1-yl}propan-2-yl)-2-phenylcyclopropanecarboxamide;EVJ; VU0359595;ML270;(1R,2R)-N-((S)-1-(4-(5-Bromo-2-oxo-2,3-dihydro-1H-benzo[d]imidazol-1-yl)piperidin-1-yl)propan-2-yl)-2-phenylcyclopropanecarboxamide;(1R,2R)-N-[(1S)-2-[4-(5-bromo-2,3-dihydro-2-oxo-1H-benzimidazol-1-yl)-1-piperidinyl]-1-methylethyl]-2-phenyl-cyclopropanecarboxamide;VU0359595-1;BDBM87119;AOB1035;cid_53470193;(1
Cas No.	1246303-14-9
分子式	C₂₅H₂₉BrN₄O₂
分子量	497.43
包装储存	4°C, sealed storage, away from moisture and light *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

生物活性

VU0359595 (CID-53361951; ML-270) is a potent and selective pharmacological phospholipase D1 (PLD1) inhibitor with an IC₅₀ of 3.7 nM. VU0359595 is >1700-fold selective for PLD1 over PLD2 (IC₅₀ of 6.4 μM). VU0359595 can be used for the research of cancer, diabetes, neurodegenerative and inflammatory diseases.

性状

Solid

IC50 & Target[1][2]

PLD1

3.7 nM (IC₅₀)

PLD2

6.4 μM (IC₅₀)

体外研究(In Vitro)

VU0359595 (5, 50, 500, 5000 nM) inhibits basal and FCS/IGF-1 stimulated proliferation of astroglial cells.
VU0359595 (5, 50, 500 nM; 30 min) does not affect basal PLD activity in astrocytes but reduces mitogen-stimulated PLD activity in a concentration-dependent manner.
VU0359595 (0.15 μM; 1 h before high glucose treatment and 4 h during high glucose treatment) partially reduces the increase [H]-phosphatidylethanol (PEth) generation induced by high glucose (33 mM) in retinal pigment epithelium (RPE) cells.
VU0359595 (5 μM; 1 h prior to LPS treatment) modulates the autophagic process of LPS-induced (10 μg/ml; 24 h) RPE cells.
VU0359595 (2 nM; pretreatment 30 min) blocks the increase of A. fumigatus internalization induced by 50 ng/ml gliotoxin in A549 cells.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature or refrigerated transportation.

储存方式

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

参考文献

[1]. Lewis JA, et al. Design and synthesis of isoform-selective phospholipase D (PLD) inhibitors. Part I: Impact of alternative halogenated privileged structures for PLD1 specificity. Bioorg Med Chem Lett. 2009;19(7):1916-1920.

[2]. Burkhardt U, et al. Phospholipase D is a target for inhibition of astroglial proliferation by ethanol. Neuropharmacology. 2014;79:1-9. [Information]

[3]. Tenconi PE, et al. High glucose-induced phospholipase D activity in retinal pigment epithelium cells: New insights into the molecular mechanisms of diabetic retinopathy. Exp Eye Res. 2019;184:243-257. [Information]

[4]. Bermúdez V, et al. Lipopolysaccharide-Induced Autophagy Mediates Retinal Pigment Epithelium Cells Survival. Modulation by the Phospholipase D Pathway. Front Cell Neurosci. 2019;13:154. Published 2019 Apr 24. [Information]

[5]. Jia X, et al. Gliotoxin promotes Aspergillus fumigatus internalization into type II human pneumocyte A549 cells by inducing host phospholipase D activation. Microbes Infect. 2014 Jun;16(6):491-501. [Information]

溶解度数据

体外研究:

DMSO : 10 mg/mL (20.10 mM; Need ultrasonic)

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.0103 mL	10.0517 mL	20.1033 mL
5 mM	0.4021 mL	2.0103 mL	4.0207 mL
10 mM	0.2010 mL	1.0052 mL	2.0103 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

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产品使用指南

Data Sheet

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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