CS-1190
| 中文名稱 | CS-1190 |
|---|---|
| 中文同義詞 | 3-均三甲苯基-3A,4,5,6,7,7A-六氫-4,7-亞甲基苯并[D]異惡唑;化合物SN 2;SN 2,TRPML3通道激活劑;化合物SN 2,10 MM DMSO 溶液 |
| 英文名稱 | SN 2 |
| 英文同義詞 | 3a,4,5,6,7,7a-Hexahydro-3-(2,4,6-trimethylphenyl)-4,7-methano-1,2-benzisoxazole;CS-1190;SN2;SN-2;4,7-Methano-1,2-benzisoxazole, 3a,4,5,6,7,7a-hexahydro-3-(2,4,6-trimethylphenyl)-;inhibit,Transient receptor potential channels,SN-2,SN 2,TRP Channel,Inhibitor,SN2;3-Mesityl-3a,4,5,6,7,7a-hexahydro-4,7-methanobenzo[d]isoxazole;SN 2, 10 mM in DMSO |
| CAS號(hào) | 823218-99-1 |
| 分子式 | C17H21NO |
| 分子量 | 255.35 |
| EINECS號(hào) | |
| 相關(guān)類別 | |
| Mol文件 | 823218-99-1.mol |
| 結(jié)構(gòu)式 |  |
CS-1190 性質(zhì)
| 沸點(diǎn) | 370.8±52.0 °C(Predicted) |
|---|---|
| 密度 | 1.27±0.1 g/cm3(Predicted) |
| 儲(chǔ)存條件 | 2-8°C |
| 溶解度 | DMSO：100 mg/mL（391.62 mM；需要超聲波） |
| 形態(tài) | 粉末 |
| 顏色 | 白色至米白色 |
EC50: 1.8±0.13 μM (TRPML3), >29.9 μM (TRPML1)
The conductance of TRPML3 channels is estimate, when activated with 10 μM SN-2 is approximately 10 pS at ?80 mV. TRPML3-expressing HEK293 cells are perfused with a series starting with compound alone (in SBS), with compound in ELS, and finally with ELS alone. Two representative compounds, SF-24 and SN-2, are tested. SF-24 is one of the least effective compounds, and SN-2 is one of the most active ones. SN-2 has a similar synergistic effect, also reaching up-to 10-fold enhancement of the combined response when compared with the individual responses, reaching average current densities of up to 3 nA/pF at ?80 mV. Dominant negative TRPML3(D458K) is highly effective in eliminating SN-2-induced activity in epidermal melanocytes, suggesting that SN-2 activates a channel that is not responsive in presence of TRPML3(D458K). Such a dominant negative action might be attributed to potential heteromerization of TRPML3(D458K) with an SN-2-responsive channel.