Free shipping on all orders over $ 500

EPPTB

Cat. No. M8504
EPPTB Structure
Size Price Availability
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

EPPTB is a selective antagonist of the trace amine-associated receptor 1 (TAAR1), a G protein-coupled receptor (GPCR) activated by endogenous trace amines (tyramine, tryptamine, synephrine, octopamine, β)-phenylethylamine), which are chemically similar to monoaminergic neurotransmitters (epinephrine, norepinephrine, dopamine). TAAR1 is considered a promising target for the treatment of neuropsychiatric disorders, however study of TAAR1 has hampered by the fact that selective ligands have not been available. EPPTB is the first potent and selective TAAR1 antagonist with an IC50 of 28 nM at mouse TAAR1. EPPTB is less selective for rat and human with IC50 values of 4539 and 7487 nM, respectively.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 378.39
Formula C20H21F3N2O2
CAS Number 1110781-88-8
Purity >98%
Solubility DMSO: 20 mg/mL
clear
Storage at -20°C
References

[1] Daniel Maia Nogueira de Oliveira, et al. Differential effects of β-methylphenylethylamine and octopamine on contractile parameters of the rat gastrointestinal tract

[2] Qingxia Kong, et al. The TAAR1 inhibitor EPPTB suppresses neuronal excitability and seizure activity in mice

[3] Elisa Landucci, et al. N-(3-Ethoxy-phenyl)-4-pyrrolidin-1-yl-3-trifluoromethyl-benzamide (EPPTB) prevents 3-iodothyronamine (T1AM)-induced neuroprotection against kainic acid toxicity

[4] Henri Stalder, et al. Selective antagonists of mouse trace amine-associated receptor 1 (mTAAR1): discovery of EPPTB (RO5212773)

[5] Amyaouch Bradaia, et al. The selective antagonist EPPTB reveals TAAR1-mediated regulatory mechanisms in dopaminergic neurons of the mesolimbic system

Related Products
SPH3127

SPH3127 is an oral direct renin inhibitor (DRI) that is being developed for hypertension. The renin-angiotensin-aldosterone system is responsible for the regulation of blood pressure.

SAFit2

SAfit2 is a potent inhibitor of FK506-binding protein 51 (FKBP51) with a Ki value of 6 nM. SAfit2 has been used as a potential agent in the study of major depression, obesity, and chronic pain.

lipid 10a

“lipid 10a” (Arcturus tunable lipid for RNA drug delivery).

BAY 1214784

BAY 1214784 is a potent, selective and orally active antagonist of the human gonadotropin-releasing hormone receptor (hGnRH-R).BAY 1214784 has the potential to be studied in uterine fibroids.

3-MORPHOLINOSYDNONIMINE

  Catalog
Abmole Inhibitor Catalog




Keywords: EPPTB supplier, inhibitors

Contact Us

Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2020 AbMole BioScience. All Rights Reserved.