Product Name :
TPC2-A1-N
Description:
TPC2-A1-N is a powerful and Ca2+-permeable agonist of two pore channel 2 (TPC2), which plays its role by mimicking the physiological actions of NAADP. TPC2-A1-P reproducibly evokes significant Ca2+ responses from TPC2 (EC50=7.8 μM), and the effect can be blocked by several TPC blockers. TPC2-A1-N can be used to probe different functions of TPC2 channels in intact cells.
CAS:
136186-07-7
Molecular Weight:
401.17
Formula:
C17H9Cl2F3N2O2
Chemical Name:
(2Z)-2-cyano-3-(3,5-dichlorophenyl)-3-hydroxy-N-[4-(trifluoromethyl)phenyl]prop-2-enamide
Smiles :
N#C/C(=C(/O)\C1C=C(Cl)C=C(Cl)C=1)/C(=O)NC1C=CC(=CC=1)C(F)(F)F
InChiKey:
FVJSEJNZNQVVDZ-PFONDFGASA-N
InChi :
InChI=1S/C17H9Cl2F3N2O2/c18-11-5-9(6-12(19)7-11)15(25)14(8-23)16(26)24-13-3-1-10(2-4-13)17(20,21)22/h1-7,25H,(H,24,26)/b15-14-
Purity:
≥98% (or refer to the Certificate of Analysis)
Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition :
Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.Oligonucleotide Synthesis
Shelf Life:
≥12 months if stored properly.
Stock Solution Storage:
0 – 4 oC for 1 month or refer to the Certificate of Analysis.
Additional information:
TPC2-A1-N is a powerful and Ca2+-permeable agonist of two pore channel 2 (TPC2), which plays its role by mimicking the physiological actions of NAADP. TPC2-A1-P reproducibly evokes significant Ca2+ responses from TPC2 (EC50=7.8 μM), and the effect can be blocked by several TPC blockers. TPC2-A1-N can be used to probe different functions of TPC2 channels in intact cells.|Product information|CAS Number: 136186-07-7|Molecular Weight: 401.17|Formula: C17H9Cl2F3N2O2|Chemical Name: (2Z)-2-cyano-3-(3,5-dichlorophenyl)-3-hydroxy-N-[4-(trifluoromethyl)phenyl]prop-2-enamide|Smiles: N#C/C(=C(/O)\C1C=C(Cl)C=C(Cl)C=1)/C(=O)NC1C=CC(=CC=1)C(F)(F)F|InChiKey: FVJSEJNZNQVVDZ-PFONDFGASA-N|InChi: InChI=1S/C17H9Cl2F3N2O2/c18-11-5-9(6-12(19)7-11)15(25)14(8-23)16(26)24-13-3-1-10(2-4-13)17(20,21)22/h1-7,25H,(H,24,26)/b15-14-|Technical Data|Appearance: Solid Power|Purity: ≥98% (or refer to the Certificate of Analysis)|Solubility: DMSO : 250 mg/mL (623.{{Amitriptyline} medchemexpress|{Amitriptyline} mAChR|{Amitriptyline} Protocol|{Amitriptyline} Purity|{Amitriptyline} manufacturer|{Amitriptyline} Epigenetic Reader Domain} 18 mM; Need ultrasonic).PMID:23558135 |Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis|Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.|Shelf Life: ≥12 months if stored properly.|Stock Solution Storage: 0 – 4 oC for 1 month or refer to the Certificate of Analysis.|Drug Formulation: To be determined|HS Tariff Code: 382200|How to use|In Vitro:|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 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 7.8 μM for TPC2-A1-N in a cell line stably expressing TPC2L11A/L12A. TPC2-A1-N (10 μM) 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 (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 (TPC2M484L) compared to the wild-type isoform, and exhibits an EC50 value of 0.6 μM for TPC2-A1-N.|Products are for research use only. Not for human use.|
