1-Oxa-4,9-diazaspiro[5.5]undecan-3-one, 9-[2-(2,5-difluorophenyl)ethyl]-4-ethyl-2-methyl-, hydrochloride (1:1), (2R)-
- CAS No.
- 2535970-65-9
- Chemical Name:
- 1-Oxa-4,9-diazaspiro[5.5]undecan-3-one, 9-[2-(2,5-difluorophenyl)ethyl]-4-ethyl-2-methyl-, hydrochloride (1:1), (2R)-
- Synonyms
- EST73502 hydrochloride;1-Oxa-4,9-diazaspiro[5.5]undecan-3-one, 9-[2-(2,5-difluorophenyl)ethyl]-4-ethyl-2-methyl-, hydrochloride (1:1), (2R)-
- CBNumber:
- CB59315762
- Molecular Formula:
- C19H27ClF2N2O2
- Molecular Weight:
- 388.88
- MDL Number:
- MFCD32878295
- MOL File:
- 2535970-65-9.mol
1-Oxa-4,9-diazaspiro[5.5]undecan-3-one, 9-[2-(2,5-difluorophenyl)ethyl]-4-ethyl-2-methyl-, hydrochloride (1:1), (2R)- Chemical Properties,Uses,Production
Uses
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].
Biological Activity
EST73502 hydrochloride 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 hydrochloride has antinociceptive activity[1]. EST73502 hydrochloride (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 hydrochloride (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].
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: | Male CD1 mice, PSNL model[1] |
| Dosage: | 5 mg/kg |
| Administration: | Intraperitoneal injection, twice a day, for 10 days |
| Result: | Attenuated the expression of mechanical allodynia induced by PSNL, reaching a maximal effect of 56%. |
References
[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.
1-Oxa-4,9-diazaspiro[5.5]undecan-3-one, 9-[2-(2,5-difluorophenyl)ethyl]-4-ethyl-2-methyl-, hydrochloride (1:1), (2R)- Preparation Products And Raw materials
Raw materials
Preparation Products
1-Oxa-4,9-diazaspiro[5.5]undecan-3-one, 9-[2-(2,5-difluorophenyl)ethyl]-4-ethyl-2-methyl-, hydrochloride (1:1), (2R)- Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| TargetMol Chemicals Inc. | +1-781-999-5354; | support@targetmol.com | United States | 39035 | 58 |
| Shanghai Yifei Biotechnology Co. , Ltd. | 021-65675885 18964387627 | customer_service@efebio.com | China | 11973 | 58 |
| TargetMol Chemicals Inc. | 15002134094 | marketing@targetmol.cn | China | 29257 | 58 |
| Biosynth Biological Technology (Suzhou) Co Ltd | 51288865780 | sales@biosynth.com | China | 6051 | 58 |
| Supplier | Advantage |
|---|---|
| TargetMol Chemicals Inc. | 58 |
| Shanghai Yifei Biotechnology Co. , Ltd. | 58 |
| TargetMol Chemicals Inc. | 58 |
| Biosynth Biological Technology (Suzhou) Co Ltd | 58 |
View Lastest Price from 1-Oxa-4,9-diazaspiro[5.5]undecan-3-one, 9-[2-(2,5-difluorophenyl)ethyl]-4-ethyl-2-methyl-, hydrochloride (1:1), (2R)- manufacturers
| Image | Update time | Product | Price | Min. Order | Purity | Supply Ability | Manufacturer | |
|---|---|---|---|---|---|---|---|---|
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2025-07-27 | EST73502 hydrochloride
2307458-82-6
|
US $228.00-1400.00 / mg | 10g | TargetMol Chemicals Inc. |
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- EST73502 hydrochloride
2307458-82-6
- US $228.00-1400.00 / mg
- TargetMol Chemicals Inc.




