KOR/DOR agonist 1 

KOR/DOR agonist 2 is a KOR and DOR opioid receptors agonist with K_i values of 0.14 nM, and 0.93 nM, respectively. KOR/DOR agonist 2 shows significant antinociceptive effects. KOR/DOR agonist 2 penetrates the blood-brain barrier^[1].

KOR/DOR agonist 2 (compound 21) has subnanomolar binding for the MOR, with a K_i of 0.20 nM^[1].
In [35S]-GTPγS-binding assay, KOR/DOR agonist 2 shows functional activity at the KOR, MOR, and DOR with an EC₅₀ values of 0.04 nM, 0.58 nM, 1.28 nM, respectively^[1].

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

KOR/DOR agonist 2 (0.1 mg/kg; subcutaneous injection; once) results in significant antinociceptive effects in a warm-water tail immersion assay^[1].

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

476.56

C₂₈H₃₂N₂O₅

O[C@]12[C@@]3(C4=C(C(O)=CC=C4C[C@H]2N(CC3)CC5CC5)O6)[C@@H]6[C@H](CC1)N(C(/C=C/C7=CC=CO7)=O)C

Room temperature in continental US; may vary elsewhere.

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

• [1]. Celsey M St Onge, et al. Systematic Structure-Activity Relationship Study of Nalfurafine Analogues toward Development of Potentially Nonaddictive Pain Management Treatments. J Med Chem. 2024 May 30.  [Content Brief]