| Identification | Back Directory | [Name]
DPTIP | [CAS]
351353-48-5 | [Synonyms]
DPTIP
Phenol, 2,6-dimethoxy-4-[4-phenyl-5-(2-thienyl)-1H-imidazol-2-yl]-
2,6-dimethoxy-4-[5-phenyl-4-(thiophen-2-yl)-1H-im
idazol-2-yl]phenol
extracellular,Inhibitor,exosome,DPTIP,Phospholipase,vesicles,inhibit,N-SMase | [Molecular Formula]
C21H18N2O3S | [MDL Number]
MFCD34470276 | [MOL File]
351353-48-5.mol | [Molecular Weight]
378.44 |
| Chemical Properties | Back Directory | [Boiling point ]
608.3±55.0 °C(Predicted) | [density ]
1.292±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
Soluble in DMSO | [form ]
Solid | [pka]
9.27±0.25(Predicted) | [color ]
Off-white to gray |
| Hazard Information | Back Directory | [Uses]
DPTIP is a potent brain penetrant neutral sphingomyelinase 2 (N-SMase 2) inhibitor (exosome inhibitor), with an IC50 of 30 nM[1][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.
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| [storage]
Store at -20°C | [References]
[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. DOI:10.1038/s41598-018-36144-2
[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. DOI:10.1080/14756366.2020.1754814 |
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