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136186-07-7

中文名稱 TPC2-A1-N
英文名稱 2-Propenamide, 2-cyano-3-(3,5-dichlorophenyl)-3-hydroxy-N-[4-(trifluoromethyl)phenyl]-
CAS 136186-07-7
分子式 C17H9Cl2F3N2O2
分子量 401.17
MOL 文件 136186-07-7.mol
更新日期 2023/03/20 15:41:27
136186-07-7 結(jié)構(gòu)式 136186-07-7 結(jié)構(gòu)式

基本信息

英文別名
TPC2-A1-N
2-Propenamide, 2-cyano-3-(3,5-dichlorophenyl)-3-hydroxy-N-[4-(trifluoromethyl)phenyl]-

物理化學(xué)性質(zhì)

沸點(diǎn)536.9±50.0 °C(Predicted)
密度1.546±0.06 g/cm3(Predicted)
儲(chǔ)存條件-20°C儲(chǔ)存
酸度系數(shù)(pKa)5.05±0.60(Predicted)
形態(tài)Solid
顏色White to off-white

常見問(wèn)題列表

生物活性
TPC2-A1-N 是一種強(qiáng)大的 Ca2+-可滲透雙孔通道 2 (TPC2) 的激動(dòng)劑,通過(guò)模擬 NAADP 的生理作用發(fā)揮作用。TPC2-A1-N 可誘導(dǎo) TPC2 顯著的 Ca2+ 響應(yīng) (EC50=7.8 μM),這種響應(yīng)并可被一些 TPC 阻斷劑阻斷。TPC2-A1-N 可用于檢測(cè)完整細(xì)胞中 TPC2 通道的不同功能。
靶點(diǎn)

EC50: 10.5 μM (Ca 2+ current response from TPC2)

體外研究

Two-pore channels (TPC1-3) are ancient members of the voltage-gated ion channel superfamily. TPCs are expressed throughout the endo-lysosomal system and regulates the trafficking of various cargoes. TPC2 can mediate different physiological and possibly pathophysiological effects depending on how it is activated.?The?ion selectivity of TPC2 is not fixed but rather agonist-dependent. TPC2 is a unique example of an ion channel that conducts different ions in response to different activating ligands.TPC2-A1-N (10 μM) reproducibly evokes Ca 2+ signals, and TPC2-A1-N response reachs its plateau faster than TPC2-A1-P. The EC 50 in full concentration-effect relationships for the plateau response is 7.8 μM for TPC2-A1-N in a cell line stably expressing TPC2 L11A/L12A .TPC2-A1-N (10 μM) evokes Ca 2+ influx through the TPC2 pore evokes Ca 2+ signals in cells expressing TPC2L11A/L12A?but not TPC2 L11A/L12A/L265P . Additionally, the responses to TPC2-A1-N can be selectively blocked by the identified TPC2 blockers Tetrandrine (HY-13764, Tet), Raloxifene (HY-13738, Ral), and Fluphenazine (HY-A0081, Flu) by removal of extracellular Ca 2+ .In endo-lysosomal patch-clamp experiments, TPC2-A1-N (30 μM) elicits currents using Na + as the major permeantion, in vacuolin-enlarged endo-lysosomes isolated from isolated from HEK293 cells transiently expressing human TPC2 (hTPC2) but not in cells expressing TPC1.In endo-lysosomal patch-clamp experiments, TPC2-A1-N (30 μM) induces larger currents in endo-lysosomes isolated from cells expressing a gain-of-function variant of TPC2 (TPC2 M484L ) compared to the wild-type isoform, and exhibits an EC 50 value of 0.6 μM for TPC2-A1-N.

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