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Opioid Receptor Antagonists

Cat.No. Product Name Information Product Use Citations Product Validations
S2722 JTC-801 JTC-801 is a selective opioid receptor-like1 (ORL1) receptor antagonist with IC50 of 94 nM, weakly inhibits receptors δ, κ, and μ.
Clin Exp Med, 2025, 26(1):11
Cancer Drug Resistance, 2025, 45
Cancer Drug Resist, 2025, 8:45
Verified customer review of JTC-801
S5935 Alvimopan Alvimopan (LY 246736, ADL 8-2698) is a potent, relatively nonselective opioid antagonist with Ki values of 0.77, 4.4, and 40 nM for the μ, δ, and κ opioid receptors, respectively, displaying >100-fold selectivity over other aminergic G-protein-coupled receptors.
Curr Issues Mol Biol, 2024, 46(7):6472-6488
E4647 Aticaprant Aticaprant (CERC-501, LY-2456302) is a potent, orally bioavailable, centrally-penetrant antagonist of the kappa opioid receptor with a Ki of 0.807 nM. It exhibits an antidepressant effect with the potential to treat major depressive disorder (MDD).
E2868 Naloxegol Oxalate Naloxegol oxalate (NKTR-118 oxalate) is a μ-opioid-receptor antagonist with a Ki of 33.8 nM. Naloxegol oxalate inhibits opioid binding in μ-opioid receptors in the gastrointestinal tract and effective for alleviating opioid-induced constipation.
E2880 methylnaltrexone bromide Methylnaltrexone bromide is an antagonist of µ-opioid receptor that reduces the viability of lung cancer cells by inhibiting Src activation.
E7162 CTAP CTAP is a potent, highly selective, and blood–brain barrier penetrant antagonist of μ opioid receptor with an IC50 of 3.5 nM. It displays over 1200-fold selectivity over δ opioid and somatostatin receptors. It exhibits anti-dyskinetic potential and can be used for the study of L-DOPA-induced dyskinesia (LID) and opiate overdose or addiction.