For research use only. Not for therapeutic Use.
EST64454 hydrochloride is a selective and orally active sigma-1 receptor antagonist with a Ki of 22 nM. EST64454 hydrochloride has the potential for the research of the pain[1].
EST64454 (10 mg/kg; p.o.; male Wistar rats) treatment shows the Cmax, t1/2, AUC0-∞, Vss and F% are 771 ng/mL, 3.4 hours, 1431 ng h/mL, 4.4 l/kg and 69%, respectively[1].
EST64454 (10 mg/kg; p.o.; male CD1 mice) treatment shows the Cmax, t1/2, AUC0-∞, Vss and F% were 1178 ng/mL, <1 hours, 2645 ng h/mL, 1.2 l/kg and 60%, respectively[1].
| Catalog Number | I027022 |
| CAS Number | 1950569-11-5 |
| Synonyms | 1-[4-[2-[[1-(3,4-difluorophenyl)pyrazol-3-yl]methoxy]ethyl]piperazin-1-yl]ethanone;hydrochloride |
| Molecular Formula | C18H23ClF2N4O2 |
| Purity | ≥95% |
| InChI | InChI=1S/C18H22F2N4O2.ClH/c1-14(25)23-8-6-22(7-9-23)10-11-26-13-15-4-5-24(21-15)16-2-3-17(19)18(20)12-16;/h2-5,12H,6-11,13H2,1H3;1H |
| InChIKey | YJZGDOPAALDWAT-UHFFFAOYSA-N |
| SMILES | CC(=O)N1CCN(CC1)CCOCC2=NN(C=C2)C3=CC(=C(C=C3)F)F.Cl |
| Reference | [1]. Díaz JL, et al. EST64454: a Highly Soluble σ1 Receptor Antagonist Clinical Candidate for Pain Management. J Med Chem. 2020;63(23):14979-14988. |
