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Tocris/EPPTB/4518/50/50 mg

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货号: 4518/50

品牌: Tocris

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Description: Trace amine 1 (TA₁) receptor antagonist/inverse agonist

Chemical Name: N-(3-Ethoxyphenyl)-4-(1-pyrrolidinyl)-3-(trifluoromethyl)benzamide

Purity: ≥99% (HPLC)

Biological Activity Technical Data Solubility Calculators Datasheets References

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

Product Datasheets

Certificate of Analysis / Product Datasheet

Safety Datasheet

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

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