Opioid Receptor Antagonist

Opioid Receptor Antagonists (112):

Cat. No.	Product Name	Effect	Purity

HY-114072

J-113397	Antagonist	99.00%
J-113397 is the first potent and selective nonpeptidyl ORL1 receptor antagonist (K_i: cloned human ORL1=1.8 nM) without any agonistic effects on other opioid receptors.

HY-101376

(+)-N-Allylnormetazocine hydrochloride	Antagonist	≥99.0%
(+)-N-Allylnormetazocine ((+)-SKF 10047) hydrochloride is a benzomorphan opioid with psychotomi metic effects. (+)-N-Allylnormetazocine hydrochloride is an opioid receptor antagonist with K_i values of 300 nM and 27 μM for σ1 and σ2 opioid receptors, respectively. (+)-N-Allylnormetazocine hydrochloride can be used for the research of neurological disease.

HY-107721

(±)-J-113397	Antagonist	98.59%
(±)-J-113397 is a potent and selective non-peptidyl ORL1 receptor antagonist with a K_i of 1.8 nM for cloned human ORL1. J-113397 inhibited nociceptin/orphanin FQ-stimulated GTPγS binding to CHO cells expressing ORL1 with an IC₅₀ value of 5.3 nM. J-113397 can be used for researching the physiological roles of nociceptin/orphanin FQ.

HY-101011

Naloxonazine dihydrochloride	Antagonist	98.1%
Naloxonazine dihydrochloride is a specific μ-opioid receptor antagonist with an IC₅₀ of 5.4 nM. Naloxonazine dihydrochloride also shows anti-leishmanial activity.

HY-13243

Alvimopan	Antagonist	98.66%
Alvimopan (ADL 8-2698) is a potent, selective, orally active and reversible μ-opioid receptor antagonist, with an IC₅₀ of 1.7 nM. Alvimopan has selectivity for μ-opioid receptor (K_i=0.47 nM) over κ- and δ-opioid receptors (K_is=100, 12 nM, respectively). Alvimopan can be used for the research of postoperative ileus.

HY-123689

Samidorphan	Antagonist	99.04%
Samidorphan (ALKS-33) is an orally active opioid system modulator that has a high affinity for binding with μ‐opioid, κ‐opioid, and δ‐opioid receptors. Samidorphan acts as an antagonist at μ‐opioid receptors and acts as a partial agonist at k-opioid and δ‐opioid receptors. Samidorphan primarily acts as an opioid receptor antagonist in vivo.

HY-107744

Nalmefene	Antagonist	99.70%
Nalmefene is a long acting opioid (MOR and DOR antagonist), and a partial KOR agonist. Nalmefene is used for opioid overdose and alcohol dependence.

HY-15708

LY2795050	Antagonist	98.68%
LY2795050 is a short-acting selective κ(kappa)-opioid receptor (KOR) antagonist. LY2795050 has high affinity for the KOR with K_i value of 0.72 nM. LY2795050 can be used for the research of central nervous system dysfunction.

HY-107748

5'-Guanidinonaltrindole hydrochloride	Antagonist	98.72%
5'-Guanidinonaltrindole (5'-GNTI) hydrochloride is a highly selective and potent κ-opioid receptor antagonist with a K_i of 0.18 nM for human κ-opioid receptor.

HY-118949

LY255582	Antagonist	≥98.0%
LY255582 is a pan-opioid antagonist and has high affinity for mu, delta, and kappa receptors (K_i: 0.4 nM, 5.2, 2.0 nM respectively). LY255582 can decrease food intake and body weight. LY255582 can be used for the research of obesity.

HY-101223

DIPPA hydrochloride	Antagonist	99.7%
DIPPA (hydrochloride) is an irreversible, long-lasting, selective and high affinity κ-opioid receptor antagonist. DIPPA (hydrochloride) can be used for the research of anxiety and antidepressant.

HY-16765A

Axelopran sulfate	Antagonist
Axelopran sulfate is an opioid receptor antagonist with pKi values of 9.8, 8.8 and 9.9 for human recombinant μ and δ receptors and guinea pig κ receptor, respectively.

HY-118416

BMS-986124	Antagonist	99.00%
BMS-986124 is a μ-opioid receptor silent allosteric modulator (μ-SAMs). BMS-986124 antagonizes positive allosteric modulator effect of BMS-986122 (µ-OR PAM).

HY-19627

Naldemedine	Antagonist
Naldemedine (S-297995) is an orally active μ-opioid receptor antagonist (PAMORA). Naldemedine shows potent binding affinities (Ki=0.34, 0.43, 0.94 nM, respectively) and antagonist activities (IC₅₀=25.57, 7.09, 16.1 nM, respectively) for recombinant human μ-, δ-, and κ- opioid receptors. Naldemedine can be used in opioid-induced constipation (OIC) research. Naldemedine is predicted to bind to 3CL^pro encoded by SARS-CoV2 genome.

HY-100122

Bevenopran	Antagonist	99.82%
Bevenopran is a peripheral μ-opioid receptor antagonist.

HY-A0118

Naloxegol	Antagonist
Naloxegol (NKTR-118; AZ-13337019) is a μ-opioid-receptor antagonist. Naloxegol inhibits opioid binding in μ-opioid receptors in the gastrointestinal tract and effective for alleviating opioid-induced constipation.

HY-107750

Cyprodime	Antagonist
Cyprodime is a selective μ opioid receptor (MOR) antagonist with K_is of 5.4, 244.6, and 2187 nM for μ, δ, and κ, respectively.

HY-135230

LY2444296	Antagonist	99.59%
LY2444296 is an orally bioavailable, high-affinity and selective short-acting kappa opioid receptor (KOPR) antagonist, with a K_i value of ～1 nM. LY2444296 exhibits anti-anxiety like effects.

HY-114072A

(S,S)-J-113397	Antagonist	99.87%
(S,S)-J-113397 is an isomer of J-113397 (HY-114072). J-113397 is an Opioid Receptor antagonist.

HY-N2304A

Methyl-6-alpha-Naltrexol	Antagonist
Methyl-6-alpha-Naltrexol is a metabolite of Methylnaltrexone (MNTX). Methylnaltrexone is a selective mu-opioid receptor antagonist and functions as a peripherally acting receptor antagonist in tissues of the gastrointestinal tract.

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