| Bioactivity | 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]. |
| Target | Ki: 64 nM (MOR), 118 nM (σ1R) |
| In Vivo | EST73502 monohydrochloride (10-40 mg/kg; p.o.) shows a dose-response analgesic effect reaching a maximum of 64% and an EC50 of 14 mg/kg in the paw pressure test in CD1 male mice[1].EST73502 monohydrochloride (5 mg/kg; i.p.; twice a day; for 10 days) attenuates partial sciatic nerve ligation (PSNL)-induced mechanical allodynia in male CD1 mice[1]. Animal Model: |
| Name | EST73502 monohydrochloride |
| CAS | 2535970-65-9 |
| Formula | C19H27ClF2N2O2 |
| Molar Mass | 388.88 |
| Appearance | Solid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| Reference | [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. |
EST73502 monohydrochloride
CAS: 2535970-65-9 F: C19H27ClF2N2O2 W: 388.88
EST73502 monohydrochloride is a selective, orally active and blood-brain barrier (BBB) penetrant dual μ-opioid receptor
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