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AB254331

EPPTB, TAAR1 antagonist

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MW 378.4 Da, Purity >99%. Novel, selective, highly potent trace amine associated receptor 1 (TAAR1) antagonist. Higher potency in mouse than rat and human (IC50 values are 28nM, 4539nM and 7487nM, respectively). Increases firing frequency of dopamine (DA)neurons in ventral tegmental area by blocking inward potassium current mediated by TAAR1, increasing DA activity on D2 receptor. Displays inverse agonism in vitro by reducing cAMP levels (IC50 =19nM).
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Chemical Structure - EPPTB, TAAR1 antagonist (AB254331)
  • Chemical Structure

Supplier Data

Chemical Structure - EPPTB, TAAR1 antagonist (AB254331)

2D chemical structure image of ab254331, EPPTB, TAAR1 antagonist

Key facts

CAS number

1110781-88-8

Purity

>99%

Form

Solid

form

Molecular weight

378.4 Da

Molecular formula

C<sub>2</sub><sub>0</sub>H<sub>2</sub><sub>1</sub>F<sub>3</sub>N<sub>2</sub>O<sub>2</sub>

PubChem

25175634

Nature

Synthetic

Solubility

Soluble in DMSO to 50mM

Biochemical name

Epptb

Biological description

Novel, selective, highly potent trace amine associated receptor 1 (TAAR1) antagonist. Higher potency in mouse than rat and human (IC50 values are 28nM, 4539nM and 7487nM, respectively). Increases firing frequency of dopamine (DA)neurons in ventral tegmental area by blocking inward potassium current mediated by TAAR1, increasing DA activity on D2 receptor. Displays inverse agonism in vitro by reducing cAMP levels (IC50 =19nM).

Canonical smiles

CCOC1=CC=CC(=C1)NC(=O)C2=CC(=C(C=C2)N3CCCC3)C(F)(F)F

InChi

InChI=1S/C20H21F3N2O2/c1-2-27-16-7-5-6-15(13-16)24-19(26)14-8-9-18(25-10-3-4-11-25)17(12-14)20(21,22)23/h5-9,12-13H,2-4,10-11H2,1H3,(H,24,26)

InChiKey

KLFVWQCQUXXLOU-UHFFFAOYSA-N

IUPAC Name

N-(3-ethoxyphenyl)-4-pyrrolidin-1-yl-3-(trifluoromethyl)benzamide

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Complementary Products

Primary Antibodies

AB150646

Anti-TAAR1 antibody

Immunohistochemistry (Formalin/PFA-fixed paraffin-embedded sections) - Anti-TAAR1 antibody (AB150646)

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Biochemicals

AB141296

Indirubin-3'-monoxime, GSK3beta inhibitor. CDK inhibitor.

Chemical Structure - Indirubin-3'-monoxime, GSK3beta inhibitor. CDK inhibitor. (AB141296)

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Biochemicals

AB141253

Sodium 4-phenylbutyrate, Histone deacetylase inhibitor

Immunocytochemistry/ Immunofluorescence - Sodium 4-phenylbutyrate, Histone deacetylase inhibitor (AB141253)

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Primary Antibodies

AB227825

Anti-GRK2 antibody [EPR22465]

RabMAb|Recombinant|KO Validated|Trial Size

Immunoprecipitation - Anti-GRK2 antibody [EPR22465] (AB227825)

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Product details

Solutions in DMSO may be stored at -20°C for up to 3 months.
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Properties and storage information

Shipped at conditions
Ambient - Can Ship with Ice
Appropriate short-term storage conditions
Ambient
Appropriate long-term storage conditions
-20°C
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Supplementary information

This supplementary information is collated from multiple sources and compiled automatically.

TAAR1 also known as Trace Amine-Associated Receptor 1 is a G-protein-coupled receptor primarily involved in the modulation of monoaminergic systems in the brain. It has an approximate molecular mass of 37 kDa. This receptor is expressed largely in the central nervous system particularly in regions such as the prefrontal cortex amygdala and hippocampus but also found in some peripheral tissues like the pancreas. TAAR1 is responsive to trace amines which are endogenous compounds structurally related to monoamine neurotransmitters.
Biological function summary

TAAR1 influences monoaminergic activity. It plays a critical role in regulating the release and reuptake of neurotransmitters like dopamine and serotonin. It does not form part of a larger receptor complex but instead exerts its influence by interacting with proteins associated with neurotransmitter release management. TAAR1's activation produces various responses depending on the cell type and neurological context impacting mood and cognition processes.

Pathways

TAAR1 signaling integrates into dopaminergic and serotonergic pathways. It modulates the activity of these pathways by altering the concentration of neurotransmitters through interacting with dopaminergic D2 receptors and serotonin transporters. This receptor operates within these pathways by providing feedback control influencing neurotransmitter dynamics critically involved in mood regulation and behavior expression.

TAAR1 connects closely to schizophrenia and depression. Studies associate its functional activity with altered monoamine levels seen in these conditions. In schizophrenia TAAR1 has connections with dopamine dysregulation with proteins such as the D2 receptor heavily implicated in pathophysiology. In depression its modulation of serotonin transporter function may impact therapeutic outcomes. Understanding TAAR1's role in these disorders helps guide the development of novel targeted therapies.
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Product protocols

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