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Medchemexpress LLC Ro 5212773 (EPPTB) | 1110781-88-8 | 99.85% | 378.39 | 100 MG
Supplier: Medchemexpress LLC HY11009850MG
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. This compound suppresses the excitability of hippocampal pyramidal neurons and reduces seizure-like events (SLEs) and seizure activity.
- Blocks TAAR1-mediated activation of an inwardly rectifying K+ current.
- Potently antagonizes cAMP production induced by activating mouse TAAR1 (IC50=27.5 nM).
- Dose-dependently reduces cAMP levels in HEK293 cells without TAAR1 agonist (IC50= 19 nM).
- More potent in antagonizing cAMP production by mouse TAAR1 compared to rat (IC50= 4539 nM) and human (IC50= 7487 nM) TAAR1.
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