中文名称: TPC2-A1-N
英文名称: TPC2-A1-N
CAS No: 136186-07-7
分子式: C17H9Cl2F3N2O2
分子量: 401.17
T11111 TPC2-A1-N ≥98% (psaitong)
包装规格:
5mg in glass bottle
溶解性:
溶于DMSO(250mg/ml超声)
产品描述:

基本信息

产品编号:

T11111

产品名称:

TPC2-A1-N

CAS:

136186-07-7

 

储存条件

粉末

-20℃

四年

 

 

分子式:

C17H9Cl2F3N2O2

溶于液体

-80℃

6个月

分子量:

401.17

-20℃

1个月

化学名: 

2-cyano-3-(3,5-Dichlorophenyl)-3-hydroxy-N-(4-(trifluoromethyl)phenyl)acrylamide

Solubility (25°C):

 

体外:

 

DMSO

 

Ethanol

 

Water

 

体内(现配现用):

 

1mg/ml表示微溶或不溶。

普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;⼀旦配成溶液,请分装保存,避免反复冻融造成的产品失效。

 

制备储备液

 

浓度

 

溶液体积

质量

 

1mg

 

5mg

 

10mg

1mM

2.4927mL

12.4635mL

24.9271mL

5mM

0.4985mL

2.4927mL

4.9854mL

10mM

0.2493mL

1.2464mL

2.4927mL

 

生物活性

产品描述

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=7.8μM),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。

靶点

EC50:10.5μM (Ca2+ current response from TPC2)

 

体外研究

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 (10μM) reproducibly evokes Ca2+ signals,and TPC2-A1-N response reachs its plateau faster than TPC2-A1-P.The EC50 in full concentration-effect relationships for the plateau response is 7.8μM for TPC2-A1-N in a cell line stably expressing TPC2L11A/L12A.TPC2-A1-N (10μM) evokes Ca2+ influx through the TPC2 pore evokes Ca2+ signals in cells expressing TPC2L11A/L12A but not TPC2L11A/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 Ca2+.In endo-lysosomal patch-clamp experiments,TPC2-A1-N (30μM) 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 (30μM) induces larger currents in endo-lysosomes isolated from cells expressing a gain-of-function variant of TPC2 (TPC2M484L) compared to the wild-type isoform, and exhibits an EC50 value of 0.6μM for TPC2-A1-N.

 

保存条件:
-20℃
UN码:
HazardClass:
危害声明:
安全说明:
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    C4=C3/X C4: LOG(C4):
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