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EST73502

Cat. No. M21317
EST73502  Structure
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Biological Activity

EST73502 is a selective, orally active, μ-opioid receptor (μ-opioid receptor/MOR) agonist and σ1 receptor (σ1R) antagonist that crosses the blood-brain barrier with Ki values of 64 nM and 118 nM for MOR and σ1R effects, respectively. EST73502 can be used in pain relief studies.

Chemical Information
Molecular Weight 352.42
Formula C19H26F2N2O2
CAS Number 1838622-25-5
Solubility (25°C) N/A
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Eva Ayet, et al. Xenobiotica. Preliminary in vitro approach to evaluate the drug-drug interaction potential of EST73502, a dual µ-opioid receptor partial agonist and σ1 receptor antagonist

[2] Mnica Garca, et al. J Med Chem. Discovery of EST73502, a Dual μ-Opioid Receptor Agonist and σ1 Receptor Antagonist Clinical Candidate for the Treatment of Pain

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Keywords: EST73502 supplier, Opioid Receptor, inhibitors, activators


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