TPC2-A1-N
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- CAS号:
- 136186-07-7
- 英文名:
- 2-Propenamide, 2-cyano-3-(3,5-dichlorophenyl)-3-hydroxy-N-[4-(trifluoromethyl)phenyl]-
- 英文别名:
- TPC2-A1-N;2-Cyano-3-(3,5-dichlorophenyl)-3-hydroxy-N-[4-(trifluoromethyl)phenyl]acrylamide;2-Propenamide, 2-cyano-3-(3,5-dichlorophenyl)-3-hydroxy-N-[4-(trifluoromethyl)phenyl]-
- 中文名:
- TPC2-A1-N
- 中文别名:
- 2-氰基-3-(3,5-二氯苯基)-3-羟基-N-[4-(三氟甲基)苯基]丙烯酰胺
- CBNumber:
- CB48119472
- 分子式:
- C17H9Cl2F3N2O2
- 分子量:
- 401.17
- MOL File:
- 136186-07-7.mol
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TPC2-A1-N化学性质
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沸点:
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536.9±50.0 °C(Predicted)
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密度:
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1.546±0.06 g/cm3(Predicted)
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储存条件:
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Store at -20°C
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酸度系数(pKa):
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5.05±0.60(Predicted)
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TPC2-A1-N性质、用途与生产工艺
TPC2-A1-N 是一种强大的 Ca2+-可渗透双孔通道 2 (TPC2) 的激动剂,通过模拟 NAADP 的生理作用发挥作用。TPC2-A1-N 可诱导 TPC2 显著的 Ca2+ 响应 (EC50=7.8 μM),这种响应并可被一些 TPC 阻断剂阻断。TPC2-A1-N 可用于检测完整细胞中 TPC2 通道的不同功能。
EC50: 10.5 μM (Ca
2+
current response from TPC2)
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.
TPC2-A1-N
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更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
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2024/04/30 | HY-131614 | TPC2-A1-N | | 1 mg | 1818元 |
2024/04/30 | HY-131614 | TPC2-A1-N | 136186-07-7 | 5mg | 4000元 |
136186-07-7, TPC2-A1-N 相关搜索:
- 2-氰基-3-(3,5-二氯苯基)-3-羟基-N-[4-(三氟甲基)苯基]丙烯酰胺
- 136186-07-7
- 2-Cyano-3-(3,5-dichlorophenyl)-3-hydroxy-N-[4-(trifluoromethyl)phenyl]acrylamide
- TPC2-A1-N
- 2-Propenamide, 2-cyano-3-(3,5-dichlorophenyl)-3-hydroxy-N-[4-(trifluoromethyl)phenyl]-