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Ro 5212773 (Synonyms: EPPTB)

Cat. No.: HY-110098 Purity: 99.14%
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
5 mg USD 90 In-stock
Estimated Time of Arrival: December 31
10 mg USD 160 In-stock
Estimated Time of Arrival: December 31
50 mg USD 699 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1120 In-stock
Estimated Time of Arrival: December 31
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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].

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

Molecular Weight

378.39

Formula

C₂₀H₂₁F₃N₂O₂

CAS No.
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 provided by MCE.
References
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Product Name:
Ro 5212773
Cat. No.:
HY-110098
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