For research use only. Not for therapeutic Use.
Ralmitaront (RO6889450) is an orally active agonist of trace amine-associated receptor 1 (TAAR1) with a EC50 value of 110.4 nM. Ralmitaront has antipsychotic, cognitively improvement, and antidepressant activity in rodents. Ralmitaront can be used as a neurosuppressant in the study of neuro-related diseases, such as schizophrenia (SCZ), schizoaffective disorder[1][2][3][4].
Ralmitaront (0-30 µM, 70 min) displays lower efficacy and slower binding kinetics than Ulotaront at TAAR1, whereas at the 5-HT1AR and the D2 R, Ralmitaront lacks demonstrable activity[1].
| Catalog Number | I045646 |
| CAS Number | 2133417-13-5 |
| Synonyms | 5-ethyl-4-methyl-N-[4-[(2S)-morpholin-2-yl]phenyl]-1H-pyrazole-3-carboxamide |
| Molecular Formula | C17H22N4O2 |
| Purity | ≥95% |
| InChI | InChI=1S/C17H22N4O2/c1-3-14-11(2)16(21-20-14)17(22)19-13-6-4-12(5-7-13)15-10-18-8-9-23-15/h4-7,15,18H,3,8-10H2,1-2H3,(H,19,22)(H,20,21)/t15-/m1/s1 |
| InChIKey | XHHXGKRFUPEPFM-OAHLLOKOSA-N |
| SMILES | CCC1=C(C(=NN1)C(=O)NC2=CC=C(C=C2)C3CNCCO3)C |
| Reference | [1]. Linda S Brady, et al. Redirecting the revolution: new developments in drug development for psychiatry. Expert Opin Drug Discov. 2019 Dec;14(12):1213-1219. [2]. Halff EF, et al. Trace amine-associated receptor 1 (TAAR1) agonism as a new treatment strategy for schizophrenia and related disorders. Trends Neurosci. 2023 Jan;46(1):60-74. [3]. Ågren R, et al. In Vitro Comparison of Ulotaront (SEP-363856) and Ralmitaront (RO6889450): Two TAAR1 Agonist Candidate Antipsychotics. Int J Neuropsychopharmacol. 2023 Sep 25;26(9):599-606. [4]. Yu J, et al. Elucidating the molecular pharmacology of trace amine-associated receptor 1 to advance antipsychotic drug discovery. Clin Transl Med. 2024 Feb;14(2):e1576. |
