[CAS NO. 1110781-88-8] Ro 5212773
PRODUCTS SPECIFICATIONS [1110781-88-8]
DESCRIPTION [1110781-88-8]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 378.39 |
| Molecular Formula | C20H21F3N2O2 |
| SMILES | O=C(NC1=CC=CC(OCC)=C1)C2=CC=C(N3CCCC3)C(C(F)(F)F)=C2 |
Summary
Ro 5212773 (EPPTB) is a potent and selective trace amine-associated receptor 1 (TAAR1) antagonist ( K i =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 (IC
50
=27.5 nM). cAMP levels are dose-dependently reduced by Ro 5212773 in HEK293 cells in the absence of TAAR1 agonist (IC
50
= 19 nM). EPPTB is significantly more potent in antagonizing cAMP production by mouse, as compared to rat (IC
50
= 4539 nM) and human (IC
50
= 7487 nM) TAAR1
[2]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
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
DMSO : 100 mg/mL ( 264.28 mM ; Need ultrasonic)
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 |
-
1.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.5 mg/mL (6.61 mM); Clear solution