1. GPCR/G Protein
  2. Trace Amine-associated Receptor (TAAR)
  3. Ro 5212773

Ro 5212773  (Synonyms: EPPTB)

Cat. No.: HY-110098 Purity: 99.14%
COA Handling Instructions

Ro 5212773 (EPPTB) is a potent and selective trace amine-associated receptor 1 (TAAR1) antagonist (Ki=0.9 nM for mouse TAAR1), with no significant effects on other TAARs. TAAR1 is a G protein-coupled receptor (GPCR) that is nonselectively activated by endogenous metabolites of amino acids.

For research use only. We do not sell to patients.

Ro 5212773 Chemical Structure

Ro 5212773 Chemical Structure

CAS No. : 1110781-88-8

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 99 In-stock
Solution
10 mM * 1 mL in DMSO USD 99 In-stock
Solid
5 mg USD 90 In-stock
10 mg USD 160 In-stock
50 mg USD 699 In-stock
100 mg USD 1120 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

Ro 5212773 (EPPTB) is a potent and selective trace amine-associated receptor 1 (TAAR1) antagonist (Ki=0.9 nM for mouse TAAR1), with no significant effects on other TAARs. TAAR1 is a G protein-coupled receptor (GPCR) that is nonselectively activated by endogenous metabolites of amino acids[1][2].

In Vitro

Ro 5212773 (EPPTB) suppresses the excitability of hippocampal pyramidal neurons. EPPTB also reduceds seizure-like events (SLEs) and seizure activity[1].
Ro 5212773 blocks the TAAR1-mediated activation of an inwardly rectifying K+ current[2].
Ro 5212773 potently antagonizes cAMP production induced by activating mouse TAAR1 with 1.5 μM β-phenylethylamine (IC50=27.5 nM). cAMP levels are dose-dependently reduced by Ro 5212773 in HEK293 cells in the absence of TAAR1 agonist (IC50= 19 nM). EPPTB is significantly more potent in antagonizing cAMP production by mouse, as compared to rat (IC50= 4539 nM) and human (IC50= 7487 nM) TAAR1[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

378.39

Formula

C20H21F3N2O2

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(NC1=CC=CC(OCC)=C1)C2=CC=C(N3CCCC3)C(C(F)(F)F)=C2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (264.28 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6428 mL 13.2139 mL 26.4278 mL
5 mM 0.5286 mL 2.6428 mL 5.2856 mL
10 mM 0.2643 mL 1.3214 mL 2.6428 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (6.61 mM); Clear solution

*All of the co-solvents are available by MedChemExpress (MCE).
Purity & Documentation
References
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Ro 5212773 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
Ro 5212773
Cat. No.:
HY-110098
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