MOR antagonist 2 hydrochloride 

MOR antagonist 2 hydrochloride is a blood-brain barrier-permeable μ-opioid receptor (MOR) antagonist, with an IC₅₀ of 28.37 nM, an EC₅₀ of 4.25 nM, and a K_i of 0.18 nM against MOR. MOR antagonist 2 hydrochloride stabilizes the inactive conformation of MOR to reduce receptor activation levels. MOR antagonist 2 hydrochloride antagonizes analgesic effects in the mouse warm-water tail-flick test. MOR antagonist 2 hydrochloride induces fewer opioid withdrawal symptoms (wet dog shakes, paw tremors) in mice with opioid withdrawal symptoms. MOR antagonist 2 hydrochloride can be used for the research of opioid use disorder^[1].

MOR antagonist 2 hydrochloride (Compound 7) (1.5 h) exhibits high binding affinity for MOR (K_i = 0.18 nM), with 16-fold selectivity over KOR (K_i = 2.93 nM) and 169-fold selectivity over DOR (K_i = 30.44 nM) in CHO cell membrane preparations^[1].
MOR antagonist 2 hydrochloride (1.5 h) acts as a low-efficacy partial agonist of MOR, with an EC₅₀ of 4.25 nM in [³⁵S]-GTPγS binding assays^[1].
MOR antagonist 2 hydrochloride exhibits high metabolic stability in human liver S9 fractions, and shows high plasma protein binding rates in both human and mouse plasma^[1].
MOR antagonist 2 hydrochloride exhibits favorable passive intestinal permeability, extremely low baseline efflux levels, and acts as a substrate for P-gp and BCRP transporters in Caco-2 cells^[1].

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

MOR antagonist 2 hydrochloride (10 mg/kg; s.c.; once) reduces MPE in warm water tail-immersed mice. It is a highly potent μ-opioid receptor antagonist with an AD₅₀ of 0.09 mg/kg^[1].
MOR antagonist 2 hydrochloride (0.1-5 mg/kg; s.c.; single administration) induces significantly fewer opioid withdrawal symptoms (wet dog shakes and paw tremors) in opioid-withdrawn mice than equivalent and higher doses of Naloxone (HY-17417A), while maintaining comparable μ-opioid receptor antagonist activity^[1].

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

523.02

C₂₈H₃₁ClN₄O₄

3075862-29-9

O[C@]12[C@@H]3N(CC4CC4)CC[C@@]15C6=C(C=CC(O)=C6O[C@H]5[C@H](CC2)NC(C7=NC=CC8=C7NC=C8)=O)C3.Cl

Room temperature in continental US; may vary elsewhere.

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

• [1]. Neel L, et al. Investigating the Landscape of C6-Azaindole Side Chain on the Epoxymorphinan Skeleton via the Nitrogen Walk Concept: A Strategy to Enhance Drug-Like Properties. J Med Chem. 2026;69(3):2330-2348.  [Content Brief]