| CAS |
No.351353-48-5 |
| 英文名称 |
DPTIP |
| 分子式 |
C21H18N2O3S |
| 分子量 |
378.44 |
| 溶解性 |
Soluble in DMSO |
| 纯度 |
≥98% |
| 外观(性状) |
Solid |
| 储存条件 |
Powder:-20℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year |
| SMILES |
COC1=CC(=CC(=C1O)OC)C2=NC(=C(N2)C3=CC=CS3)C4=CC=CC=C4 |
| InChIKey |
JMXVHYPSBANVAQ-UHFFFAOYSA-N |
| InChI |
InChI=1S/C21H18N2O3S/c1-25-15-11-14(12-16(26-2)20(15)24)21-22-18(13-7-4-3-5-8-13)19(23-21)17-9-6-10-27-17/h3-12，24H，1-2H3，(H，22，23) |
| PubChem CID |
1131802 |
| 靶点 |
N-SMase 2 |
| 通路 |
Metabolic Enzyme&Protease |
| 背景说明 |
DPTIP 是有效的、可透过血脑屏障的中性鞘磷脂酶(N-SMase 2)抑制剂 (外泌体抑制剂)。 |
| 生物活性 |
DPTIP is a potent brain penetrant neutral sphingomyelinase 2 (N-SMase 2) inhibitor (exosome inhibitor)， with an IC50 of 30 nM[1][2]. |
| In Vitro |
DPTIP blocks EV secretion in a dose dependent manner (0.03-30 μM)， and at 30 μM， this compound could decrease exosome release by 50% in astrocytes[2]. |
| In Vivo |
DPTIP potently (10?mg/kg IP) inhibits IL-1β-induced astrocyte-derived EV release[1].Animal Model: Mice[1].Dosage:10?mg/kg.Administration: IP 0.5?h prior to IL-1β striatal injection.Result:Brain concentrations of DPTIP are above its IC50 for nSMase2 inhibition for at least 4?h after compound administration.The number of astrocyte-derived EVs was reduced by 51?±?13% 2?h post IL-1β administration. |
| 数据来源文献 |
[1]. Camilo Rojas， et al. DPTIP， a newly identified potent brain penetrant neutral sphingomyelinase 2 inhibitor， regulates astrocyte-peripheral immune communication following brain inflammation. Sci Rep. 2018 Dec 7;8(1):17715.
[2]. Huarui Zhang， et al. Advances in the discovery of exosome inhibitors in cancer. J Enzyme Inhib Med Chem. 2020 Dec;35(1):1322-1330. |
| 规格 |
1mg 5mg 10mg 25mg |
| 单位 |
瓶 |
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