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EPPTB | TAAR1 antagonist

CAS:
1110781-88-8
Catalog Number:
10-1199
Activity:
TAAR1 antagonist
Chemical Name:
N-(3-Ethoxy-phenyl)-4-pyrrolidin-1-yl-3-trifluoromethyl-benzamide
Molecular Weight:
378.4
Molecular Formula:
C20H21F3N2O2
Solubility:
Soluble in DMSO (up to 25 mg/ml).
Physical Properties:
White solid
Purity:
99% by TLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT

EPPTB (1110781-88-8) is a novel selective trace amine associated receptor 1 (TAAR1) antagonist (IC50=28 nM at mouse TAAR1).1,2 A useful tool for probing the physiologic role of TAAR1.3-6

References/Citations:

1) Bradaia et al. (2009), The selective antagonist EPPTB reveals TAAR1-mediated regulatory mechanisms in dopaminergic neurons of the mesolimbic system; Proc. Natl. Acad. Sci. USA, 106 20081
2) Stalder et al. (2011), Selective antagonists of mouse trace amine-associated receptor 1 (mTAAR1): discovery of EPPTB (RO5212773); Bioorg. Med. Chem. Lett., 21 1227
3) Zhang et al. (2018), Striatal Tyrosine Is Stimulated via TAAR1 by 3-Iodothyronamine, But Not by Tyramine or β-Phenylethylamine; Front. Pharmacol., 9 166
4) De Greggrio et al. (2016), The hallucinogen d-lysergic diethylamide (LSD) decreases dopamine firing activity through 5-HT1A, D2 and TAAR1 receptors; Pharmacol. Res., 113 81
5) Cichero et al. (2014), Further insights into the pharmacology of the human trace amine-associated receptors: discovery of the novel ligands for TAAR1 by a virtual screening approach; Chem. Biol. Drug Des., 84 712
6) Liu et al. (2014), Ractopamine, a livestock feed additive, is a full agonist at trace amine-associated receptor 1; J. Pharmacol. Exp. Ther. 350 124

EPPTB | TAAR1 antagonist is also available in the Cellular Metabolism Library.
CAS:
1110781-88-8
Catalog Number:
10-1199
Activity:
TAAR1 antagonist
Chemical Name:
N-(3-Ethoxy-phenyl)-4-pyrrolidin-1-yl-3-trifluoromethyl-benzamide
Molecular Weight:
378.4
Molecular Formula:
C20H21F3N2O2
Solubility:
Soluble in DMSO (up to 25 mg/ml).
Physical Properties:
White solid
Purity:
99% by TLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT

Safety Data Sheet:

Product Data Sheet:

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