VU0359595

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

VU0359595 (CID-53361951; ML-270) 是一种选择性磷脂酶 D1 (PLD1) 抑制剂，IC50 值为 3.7 nM。VU0359595 对 PLD1 的选择性比 PLD2 (IC50=6.4 μM) 高 1700 倍以上。VU0359595 可用于癌症、糖尿病、神经退行性疾病和炎性疾病等疾病研究。

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.

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 [3H]-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.

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Metabolic Enzyme/Protease

Phospholipase

Phospholipase

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1246303-14-9

497.43

C25H29BrN4O2

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 10 mg/mL (20.10 mM; 超声助溶 )

C[C@@H](CN1CCC(CC1)n1c2ccc(Br)cc2[nH]c1=O)NC(=O)[C@@H]1C[C@H]1c1ccccc1

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(-20℃)

With Ice Pack

≥ 2 years