2. GPCR/G Protein Neuronal Signaling
  3. Opioid Receptor Sigma Receptor
  4. EST73502

EST73502 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 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.

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EST73502 Chemical Structure

EST73502 Chemical Structure

CAS No. : 1838622-25-5

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EST73502 Related Antibodies

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Description

EST73502 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 has antinociceptive activity[1].

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.
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
References
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EST73502 Related Classifications

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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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