Biological Activity
Trace amine 1 (TA1) receptor antagonist/inverse agonist; exhibits a higher potency at the mouse TA1 receptor than the rat and human TA1 receptors (IC50 values are 27.5, 4539 and 7487 nM, respectively). Blocks the TA1 receptor-mediated activation of an inwardly rectifying K+ current, which increases the firing frequency of dopamine (DA) neurons in the ventral tegmental area. Increases DA potency at the D2 receptor. Also displays inverse agonism, reducing basal cAMP levels in vitro (IC50 = 19 nM).
Compound Libraries
EPPTB is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 378.39 |
| Formula | C20H21F3N2O2 |
| Storage | Store at +4°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 1110781-88-8 |
| PubChem ID | 25175634 |
| InChI Key | KLFVWQCQUXXLOU-UHFFFAOYSA-N |
| Smiles | O=C(NC3=CC(OCC)=CC=C3)C1=CC(C(F)(F)F)=C(N2CCCC2)C=C1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 37.84 | 100 | |
| ethanol | 37.84 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 378.39. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.64 mL | 13.21 mL | 26.43 mL |
| 5 mM | 0.53 mL | 2.64 mL | 5.29 mL |
| 10 mM | 0.26 mL | 1.32 mL | 2.64 mL |
| 50 mM | 0.05 mL | 0.26 mL | 0.53 mL |
Molarity Calculator
Reconstitution Calculator
Dilution Calculator
Product Datasheets
References
References are publications that support the products' biological activity.
Bradaia et al (2009) The selective antagonist EPPTB reveals TAAR1-mediated regulatory mechanisms in dopaminergic neurons of the mesolimbic system. Proc.Natl.Acad.Sci.U.S.A. 106 20081 PMID: 19892733
Keywords: EPPTB, supplier, Parkinson's, disease, trace, amine-associated, receptors, 1, TAAR1, antagonists, dopamine, neurons, neurones, TA1, Trace, Amine, 1, Receptor, Trace, Amine, 1, Receptor, Tocris Bioscience
