EST73502 (monohydrochloride)

EST73502 monohydrochloride is a selective, orally active and blood-brain barrier (BBB) penetrant dual μ-opioid receptor (MOR) agonist and σ1 receptor (σ1R) antagonist, with Kis of 64 nM and 118 nM for MOR and σ1R, respectively. EST73502 monohydrochloride has antinociceptive activity[1].

Product Specifications

CAS Number

[2535970-65-9]

UNSPSC

12352005

Target

Opioid Receptor; Sigma Receptor

Type

Reference compound

Related Pathways

GPCR/G Protein; Neuronal Signaling

Applications

Neuroscience-Neuromodulation

Field of Research

Neurological Disease

Assay Protocol

https://www.medchemexpress.com/est73502-monohydrochloride.html

Purity

99.58

Solubility

DMSO : 50 mg/mL (ultrasonic)

Smiles

FC1=CC=C(F)C=C1CCN(CC2)CCC2(O[C@@H]3C)CN(CC)C3=O.[H]Cl

Molecular Formula

C19H27ClF2N2O2

Molecular Weight

388.88

References & Citations

[1]Mónica García, et al. Discovery of EST73502, a Dual μ-Opioid Receptor Agonist and σ 1 Receptor Antagonist Clinical Candidate for the Treatment of Pain. J Med Chem. 2020 Oct 16.