Opioid Receptor Antagonist

Opioid Receptor Antagonists (58):

Cat. No.	Product Name	Effect	Purity

HY-101718

Aticaprant	Antagonist	99.87%
Aticaprant (CERC-501) is a potent and centrally-penetrant kappa opioid receptor antagonist with a K_i of 0.807 nM.

HY-17417

Naloxone hydrochloride	Antagonist	99.96%
Naloxone hydrochloride is an antagonist of Opioid receptor. Naloxone hydrochloride alleviates opioid-overdose-induced respiratory depression. Naloxone hydrochloride may cause pulmonary edema and cardiac arrhythmias.

HY-101302

Naltriben mesylate	Antagonist	99.65%
Naltriben mesylate is a potent δ2-opioid receptor antagonist and a TRPM7 activator. Naltriben mesylate shows K_i values of 0.013 nM, 19 nM and 152 nM for δ, μ and κ receptors, respectively. Naltriben mesylate enhances glioblastoma cell migration and invasion. Naltriben mesylate can be used in research into neurological diseases and cancer.

HY-10487

JDTic dihydrochloride	Antagonist	98.01%
JDTic (dihydrochloride) is a potent antagonist of kappa-opioid receptors (KOR), blocking the κ-agonist U50, 488-induced antinociception.

HY-137279

Naloxone methiodide	Antagonist	99.7%
Naloxone methiodide is a peripherally restricted, nonselective, and competitive opioid receptor antagonist. Naloxone methiodide does not penetrate the blood-brain barrier.

HY-13222

BAN ORL 24	Antagonist	99.68%
BAN ORL 24 is a nociceptin/orphanin FQ (N/OFQ) peptide receptor (NOP) antagonist. BAN ORL 24 has antagonistic effect for nociceptin (NOP) receptor with K_I value of 0.24 nM in CHO cell. BAN ORL 24 can be used for the research of cancer and analgesic.

HY-P1299A

UFP-101 TFA	Antagonist	99.74%
UFP-101 TFA is a potent, selective, and competitive antagonist of the N/OFQ peptide (NOP) receptor, with a pK_i of 10.24. UFP-101 TFA displays >3000-fold selectivity over δ, μ and κ opioid receptors. UFP-101 TFA shows antidepressant-like effect.

HY-136208

TAN-452	Antagonist	99.44%
TAN-452 is an orally active, selective peripherally acting δ-opioid receptor (DOR) antagonist with a K_i of 0.47 nM and a K_b of 0.21 nM. TAN-452 is an antagonist for μ-opioid receptor (MOR; K_i=36.56 nM and K_b=9.43 nM) and κ-opioid receptor (KOR; K_i=5.31 nM and K_b=7.18 nM). TAN-452, a derivative of Naltrindole, demonstrates low brain penetrability and attenuates morphine-induced side effects without affecting pain control.

HY-76711

Naltrexone	Antagonist	99.94%
Naltrexone is an antagonist of Opioid receptor. Naltrexone inhibits cell proliferation in vivo. Naltrexone reduces tumor growth by interfering with cell signalling and modifying the immune system.

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-A0118A

Naloxegol oxalate	Antagonist	99.91%
Naloxegol oxalate (NKTR-118 oxalate; AZ-13337019 oxalate) is a μ-opioid-receptor antagonist. Naloxegol oxalate inhibits opioid binding in μ-opioid receptors in the gastrointestinal tract and effective for alleviating opioid-induced constipation.

HY-117040

nor-Binaltorphimine	Antagonist	98.20%
nor-Binaltorphimine is a selective antagonist of kappa-opioid receptor. nor-Binaltorphimine has a long-lasting effect in vivo.

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-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-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-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-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.

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