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Art. -Nr.: HY-134189

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EST73502

Name: EST73502
Brand: MedChemExpress
SKU: HY-134189
Availability: PreOrder

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.

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CAS. Nr.: 1838622-25-5
Formel: C₁₉H₂₆F₂N₂O₂
Molecular Weight:352.42

Speicherung:

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

Data Sheet (269 KB)

EST73502 Chemical Structure

CAS. Nr.: 1838622-25-5

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Other In-stock Forms of EST73502

EST73502 monohydrochloride

Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

Ki: 64 nM (MOR), 118 nM (σ1R)^[1]

Alle Opioid Receptor Isoform-spezifische Produkte anzeigen :

Alle Sigma Receptor Isoform-spezifische Produkte anzeigen :

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%.

Chemical Information

CAS. Nr. 1838622-25-5
Molecular Weight 352.42
Formel C₁₉H₂₆F₂N₂O₂
SMILES

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

Room temperature in continental US; may vary elsewhere.
Speicherung

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (269 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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MOQ

Minimum order quantity

100 mg

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vivo
Chemical Information
Reinheit & Dokumentation
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EST73502

Other In-stock Forms of EST73502

Alle Opioid Receptor Isoform-spezifische Produkte anzeigen

Alle Sigma Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Beschreibung

IC50 & Target

In Vivo

Chemical Information

Reinheit & Dokumentation

Verweise

Calculators

Help & FAQs

EST73502 Related Classifications

HY-134189 Related Classifications

Bioz

Keywords

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