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。
| 生物活性 | VU0359595 (CID-53361951; ML-270) is a potent and selective pharmacologicalphospholipaseD1 (PLD1) inhibitor with anIC50of 3.7 nM. VU0359595 is >1700-fold selective for PLD1 over PLD2 (IC50of 6.4 μM). VU0359595 can be used for the research ofcancer, diabetes, neurodegenerative and inflammatory diseases[1][2][3][4]. |
| IC50& Target[1] | PLD1 3.7 nM (IC50) | PLD2 6.4 μM (IC50) |
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体外研究
(In Vitro) | VU0359595 (5, 50, 500, 5000 nM) inhibits basal and FCS/IGF-1 stimulated proliferation of astroglial cells[2].
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[2].
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[3].
VU0359595 (5 μM; 1 h prior to LPS treatment) modulates the autophagic process of LPS-induced (10 μg/ml; 24 h) RPE cells[4].
VU0359595 (2 nM; pretreatment 30 min) blocks the increase ofA. fumigatusinternalization induced by 50 ng/ml gliotoxin in A549 cells[5].
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 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) |
| 溶解性数据 | In Vitro: DMSO : 10 mg/mL(20.10 mM;Need ultrasonic) 配制储备液 | 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 |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，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℃, 6 months; -20℃, 1 month (sealed storage, away from moisture and light)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 |
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