EPPTB

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Cat.No. 4518 - EPPTB | C20H21F3N2O2 | CAS No. 1110781-88-8
Description: Trace amine 1 (TA1) receptor antagonist/inverse agonist
Chemical Name: N-(3-Ethoxyphenyl)-4-(1-pyrrolidinyl)-3-(trifluoromethyl)benzamide
Purity: ≥99% (HPLC)
Datasheet
Citations
Reviews
Literature

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

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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

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References

References are publications that support the biological activity of the product.

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


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Citations for EPPTB

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