EST73502

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

At equivalent molar concentrations, both the salt and free forms of a compound exhibit comparable biological activity. Nevertheless, the salt form (EST73502 monohydrochloride) usually boasts enhanced water solubility and stability.

For research use only. We do not sell to patients.

EST73502 Chemical Structure

CAS No. : 1838622-25-5

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Other Forms of EST73502:

EST73502 monohydrochloride Get quote

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•Related Small Molecules:

•Related Proteins:

View All Opioid Receptor Isoform Specific Products:

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μ Opioid Receptor/MOR κ Opioid Receptor/KOR δ Opioid Receptor/DOR NOP Receptor/ORL1

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Sigma 1 Receptor Sigma 2 Receptor

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

Ki: 64 nM (MOR), 118 nM (σ1R)^[1]

In Vivo

EST73502 (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 (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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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%.

Molecular Weight

352.42

Formula

C₁₉H₂₆F₂N₂O₂

CAS No.

1838622-25-5

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

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. [Content Brief]

EST73502 Related Classifications

Neurological Disease

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Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

EST735021838622-25-5EST 73502EST-73502Opioid ReceptorSigma ReceptoranalgesicacutechronicpainantinociceptionInhibitorinhibitorinhibit

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