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KOR agonist 4

KOR agonist 4 (compound 39) is an agonist of Kappa Opioid Receptor. KOR agonist 4 is an activator of G-protein signaling. KOR agonist 4 binds with GTPγS with an EC50 of 14 nM and with an Emax of 83 %. KOR agonist 4 demonstrates moderate to high intrinsic clearance in human hepatocytes. KOR agonist 4 exhibits 60- and 810-fold selectivities versus the related mu (MOR) and delta (DOR) opioid receptors. KOR agonist 4 is potential for central nervous system (CNS) disorders research[1].

Product Specifications

UNSPSC

12352005

Target

Opioid Receptor

Related Pathways

GPCR/G Protein; Neuronal Signaling

Applications

Neuroscience-Neuromodulation

Smiles

C1(C=C(CCN(CC2CC2)CCC3=CC=CC=C3)C=C4)=C4N=CN1

Molecular Formula

C21H25N3

Molecular Weight

319.44

References & Citations

[1]Schrader TO, et al. Novel tertiary diarylethylamines as functionally selective agonists of the kappa opioid receptor. Bioorg Med Chem Lett. 2025 Jan 24;120:130111.

Shipping Conditions

Room temperature

Scientific Category

Reference compound1

Clinical Information

No Development Reported

Isoform

δ Opioid Receptor/DOR; κ Opioid Receptor/KOR; μ Opioid Receptor/MOR

Curated Selection

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